Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

Rosiglitazone [122320-73-4]

Imprimer

Référence HY-17386-50mg

Conditionnement : 50mg

Marque : MedChemExpress

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Description

Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM), with blood-brain barrier permeability. Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer^[1]^[2]^[4]^[7]^[8].

IC₅₀ & Target^[1]^[2]^[4]

PPARγ

40 nM (Kd)

PPARγ

60 nM (EC₅₀)

TRPC5

30 μM (EC₅₀)

TRPM3

Cellular Effect

Cell Line	Type	Value	Description	References
3T3-L1	EC₅₀	0.12 μM Compound: Rosiglitazone	Antidiabetic activity in mouse 3T3L1 preadipocytes assessed as increase in triglycerides level after 6 days Antidiabetic activity in mouse 3T3L1 preadipocytes assessed as increase in triglycerides level after 6 days	[PMID: 32130008]
3T3-L1	EC₅₀	1.72 μM Compound: 1; Rosi	Induction of insulin-stimulated 2-NBDG uptake in TNF-alpha-induced insulin resistant mouse 3T3L1 cells preincubated for 48 hrs followed by 2-NBDG addition measured after 30 mins in presence of insulin by fluorescence assay Induction of insulin-stimulated 2-NBDG uptake in TNF-alpha-induced insulin resistant mouse 3T3L1 cells preincubated for 48 hrs followed by 2-NBDG addition measured after 30 mins in presence of insulin by fluorescence assay	[PMID: 30481687]
BHK-21	EC₅₀	0.45 μM Compound: RSG	Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay	[PMID: 19349176]
CHO	IC₅₀	29.5 μM Compound: 1; Rosi	Inhibition of human ERG expressed in CHO cells by patch clamp assay Inhibition of human ERG expressed in CHO cells by patch clamp assay	[PMID: 30481687]
CHO-K1	EC₅₀	0.1 μM Compound: Rosiglitazone	Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay	[PMID: 20527969]
COS-1	EC₅₀	0.02 μM Compound: Rosiglitazone	In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells	[PMID: 12729668]
COS-1	EC₅₀	0.02 μM Compound: Rosiglitazone	In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells	[PMID: 12873517]
COS-1	EC₅₀	0.023 μM Compound: Rosiglitazone	In vitro maximal activation of human Peroxisome proliferator activated receptor gamma in COS-1 cell transactivation assay In vitro maximal activation of human Peroxisome proliferator activated receptor gamma in COS-1 cell transactivation assay	[PMID: 15603954]
COS-1	EC₅₀	0.12 μM Compound: Rosiglitazone	Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay	[PMID: 22197396]
COS-1	EC₅₀	20 nM Compound: Rosiglitazone	Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay	[PMID: 19530681]
COS-1	EC₅₀	20 nM Compound: rosiglitazone	Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay	[PMID: 19507861]
COS-1	EC₅₀	21 nM Compound: Rosiglitazone	Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor	[PMID: 12617924]
COS-1	EC₅₀	48 nM Compound: BRL	Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis	[PMID: 22051054]
COS-1	EC₅₀	> 1000 nM Compound: BRL	Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay	[PMID: 22051054]
COS-1	EC₅₀	> 1000 nM Compound: BRL	Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis	[PMID: 22051054]
COS-1	EC₅₀	> 3 μM Compound: Rosiglitazone	In vitro agonist activity tested for transactivation in human PPAR alpha-Gal4 chimeric COS-1 cells In vitro agonist activity tested for transactivation in human PPAR alpha-Gal4 chimeric COS-1 cells	[PMID: 12729668]
COS-1	EC₅₀	> 3 μM Compound: Rosiglitazone	In vitro agonist activity tested for transactivation in human PPAR delta-GAL4 chimeric COS-1 cells In vitro agonist activity tested for transactivation in human PPAR delta-GAL4 chimeric COS-1 cells	[PMID: 12729668]
COS-1	EC₅₀	> 3 μM Compound: Rosiglitazone	In vitro transactivation of human Peroxisome proliferator activated receptor alpha measured in PPAR-GAL4 chimeric COS-1 cell In vitro transactivation of human Peroxisome proliferator activated receptor alpha measured in PPAR-GAL4 chimeric COS-1 cell	[PMID: 12873517]
COS-1	EC₅₀	> 3 μM Compound: Rosiglitazone	In vitro transactivation of human Peroxisome proliferator activated receptor delta measured in PPAR-GAL4 chimeric COS-1 cells In vitro transactivation of human Peroxisome proliferator activated receptor delta measured in PPAR-GAL4 chimeric COS-1 cells	[PMID: 12873517]
COS-1	EC₅₀	> 3000 nM Compound: Rosiglitazone	Agonist activity at human PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay Agonist activity at human PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay	[PMID: 19530681]
COS-1	EC₅₀	> 3000 nM Compound: Rosiglitazone	Agonist activity at mouse PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay Agonist activity at mouse PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay	[PMID: 19530681]
COS-7	EC₅₀	0.03 μM Compound: 4	Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay	[PMID: 20138762]
COS-7	EC₅₀	0.043 μM Compound: Rosiglitazone	Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay	[PMID: 21873070]
COS-7	EC₅₀	0.1 μM Compound: 4	Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay	[PMID: 20138762]
COS-7	EC₅₀	> 10 μM Compound: 4	Agonist activity at human recombinant PPARalpha LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay Agonist activity at human recombinant PPARalpha LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay	[PMID: 20138762]
CV-1	EC₅₀	0.03 μM Compound: rosiglitazone	Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs	[PMID: 17507225]
CV-1	EC₅₀	0.033 μM Compound: rosiglitazone	Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18826205]
CV-1	EC₅₀	0.06 μM Compound: 6	In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells	[PMID: 8576907]
CV-1	EC₅₀	0.076 μM Compound: rosiglitazone	Transactivation of PPARgamma in CV1 cells Transactivation of PPARgamma in CV1 cells	[PMID: 16821769]
CV-1	EC₅₀	0.1 μM Compound: Rosiglitazone	Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay	[PMID: 21112784]
CV-1	EC₅₀	0.1 μM Compound: Rosiglitazone	Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay	[PMID: 21515063]
CV-1	EC₅₀	3.46 μM Compound: rosiglitazone	Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs	[PMID: 17507225]
CV-1	EC₅₀	3.46 μM Compound: rosiglitazone	Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18826205]
CV-1	EC₅₀	308 nM Compound: 3, Rosigilitazone	Activity at human PPARgamma in CV1 cells Activity at human PPARgamma in CV1 cells	[PMID: 17005394]
CV-1	EC₅₀	308 nM Compound: Rosiglitazone	Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay	[PMID: 16970391]
CV-1	EC₅₀	308 nM Compound: rosiglitazone	Agonist activity at PPARgamma in CV1 cells by transactivation assay Agonist activity at PPARgamma in CV1 cells by transactivation assay	[PMID: 17129725]
CV-1	EC₅₀	308 nM Compound: rosiglitazone	Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay	[PMID: 18029178]
CV-1	EC₅₀	325 nM Compound: BRL-49653, rosiglitazone	In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined	[PMID: 12954061]
CV-1	EC₅₀	43 nM Compound: Rosiglitazone	Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay. Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay.	[PMID: 11720854]
CV-1	EC₅₀	50 nM Compound: 1	Tested for transactivation of human PPAR gamma-Gal4 chimera in CV-1 cells Tested for transactivation of human PPAR gamma-Gal4 chimera in CV-1 cells	10.1016/S0960-894X(97)10017-8
CV-1	EC₅₀	> 10 μM Compound: Rosiglitazone	Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay	[PMID: 21112784]
CV-1	EC₅₀	> 10 μM Compound: Rosiglitazone	Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay	[PMID: 21112784]
CV-1	EC₅₀	> 10 μM Compound: Rosiglitazone	Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay	[PMID: 21515063]
CV-1	EC₅₀	> 10 μM Compound: Rosiglitazone	Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay	[PMID: 21515063]
DU-145	IC₅₀	16 μM Compound: Rosiglitazone	Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24996143]
HEK293	EC₅₀	0.004 μM Compound: Rosiglitazone	Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay	[PMID: 23286787]
HEK293	EC₅₀	0.03 μM Compound: rosiglitazone	Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay	[PMID: 24955889]
HEK293	EC₅₀	0.035 μM Compound: Rosiglitazone	Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay	[PMID: 20299214]
HEK293	EC₅₀	0.035 μM Compound: rosiglitazone	Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay	[PMID: 17292606]
HEK293	EC₅₀	0.039 μM Compound: Rosiglitazone	Transactivation of human PPARgamma expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay Transactivation of human PPARgamma expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay	10.1039/C5MD00151J
HEK293	EC₅₀	0.045 μM Compound: rosiglitazone	Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay	[PMID: 18291645]
HEK293	EC₅₀	0.1 μM Compound: 1, Avandia	Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 23294830]
HEK293	EC₅₀	0.12 μM Compound: Rosiglitazone	Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction	[PMID: 18029176]
HEK293	EC₅₀	0.19 μM Compound: Rosiglitazone	Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay	[PMID: 18029176]
HEK293	EC₅₀	0.26 μM Compound: Rosiglitazone	Agonist activity at GAL4-tagged human PPARgamma ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at GAL4-tagged human PPARgamma ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 27591006]
HEK293	EC₅₀	0.26 μM Compound: Rosiglitazone	Agonist activity at N-terminal Gal4 fused human PPARgamma LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at N-terminal Gal4 fused human PPARgamma LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 27622746]
HEK293	EC₅₀	0.3 μM Compound: Rosiglitazone	Agonist activity at GAL4N fused human PPARgamma LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay Agonist activity at GAL4N fused human PPARgamma LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay	[PMID: 28539218]
HEK293	EC₅₀	0.31 μM Compound: rosiglitazone	Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay	[PMID: 17343371]
HEK293	EC₅₀	1.1 μM Compound: 2	Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 28465099]
HEK293	EC₅₀	10 nM Compound: RGZ	Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 25305688]
HEK293	EC₅₀	10.58 μM Compound: Rosiglitazone	Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay	[PMID: 20299214]
HEK293	EC₅₀	43 nM Compound: Rosiglitazone	Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay	[PMID: 21128600]
HEK293	EC₅₀	43.71 μM Compound: Rosiglitazone	Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay	[PMID: 23265844]
HEK293	EC₅₀	> 10 μM Compound: rosiglitazone	Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay	[PMID: 17343371]
HEK293	EC₅₀	> 5 μM Compound: rosiglitazone	Agonist activity at PPARalpha in HEK293 cells by GAL4 transactivation assay Agonist activity at PPARalpha in HEK293 cells by GAL4 transactivation assay	[PMID: 18291645]
HEK293	IC₅₀	22 μM Compound: 2	Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay	[PMID: 28465099]
HT-29	IC₅₀	45 μM Compound: rosiglitazone	Antiproliferative activity against human HT29 cell line Antiproliferative activity against human HT29 cell line	[PMID: 16821769]
HUVEC	IC₅₀	1.1 μM Compound: Rosiglitazone	Anti-inflammatory activity in HUVEC assessed as reduction in TNFalpha-stimulated neutrophil-HUVEC interactions by measuring decrease in mononuclear leukocyte to endothelial cells pretreated for 20 hrs before TNFalpha stimulation for 24 hrs using freshly isolated mononuclear leukocytes perfused over endothelial monolayers for 5 mins by phase contrast microscopy Anti-inflammatory activity in HUVEC assessed as reduction in TNFalpha-stimulated neutrophil-HUVEC interactions by measuring decrease in mononuclear leukocyte to endothelial cells pretreated for 20 hrs before TNFalpha stimulation for 24 hrs using freshly isolated mononuclear leukocytes perfused over endothelial monolayers for 5 mins by phase contrast microscopy	[PMID: 31268307]
HeLa	EC₅₀	15 nM Compound: 1	Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay	[PMID: 19275963]
HeLa	EC₅₀	> 10000 nM Compound: 1	Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay	[PMID: 19275963]
HeLa	EC₅₀	> 10000 nM Compound: 1	Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay	[PMID: 19275963]
HepG2	EC₅₀	0.002 μM Compound: Rosiglitazone	Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay	[PMID: 23502212]
HepG2	EC₅₀	0.01 μM Compound: Rosiglitazone	Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay	[PMID: 23502212]
HepG2	EC₅₀	0.02 μM Compound: Rosi	Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay	[PMID: 22081932]
HepG2	EC₅₀	0.039 μM Compound: Rosiglitazone	Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay	[PMID: 18835719]
HepG2	EC₅₀	0.039 μM Compound: Rosiglitazone	Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay	[PMID: 25462281]
HepG2	EC₅₀	0.039 μM Compound: rosiglitazone	Effective concentration against human PPARgamma expressed in HepG2 cells Effective concentration against human PPARgamma expressed in HepG2 cells	[PMID: 16107150]
HepG2	EC₅₀	0.039 μM Compound: rosiglitazone	Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay	[PMID: 19775169]
HepG2	EC₅₀	0.039 μM Compound: rosiglitazone	Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay	[PMID: 23171045]
HepG2	EC₅₀	0.04 μM Compound: Rosiglitazone	Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay	[PMID: 19053776]
HepG2	EC₅₀	0.04 μM Compound: Rosiglitazone	Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay	[PMID: 25497132]
HepG2	EC₅₀	0.04 μM Compound: Rosiglitazone	Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells at 100 nM to 100 uM incubated for 20 to 22 hrs by luciferase reporter gene assay Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells at 100 nM to 100 uM incubated for 20 to 22 hrs by luciferase reporter gene assay	[PMID: 30996794]
HepG2	EC₅₀	0.043 μg/mL Compound: Rosiglitazone	Activation of PPAR in human HepG2 cells after 24 hrs by luciferase reporter gene assay Activation of PPAR in human HepG2 cells after 24 hrs by luciferase reporter gene assay	[PMID: 22364952]
HepG2	EC₅₀	0.05 μM Compound: Rosiglitazone	Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control	[PMID: 18625559]
HepG2	EC₅₀	0.158 μM Compound: Rosiglitazone	Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay	[PMID: 16979341]
HepG2	EC₅₀	0.158 μM Compound: rosiglitazone	Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay	[PMID: 16973358]
HepG2	EC₅₀	0.223 μM Compound: 1, Rosi	Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay	[PMID: 18394907]
HepG2	EC₅₀	0.223 μM Compound: 3	Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay	[PMID: 19783444]
HepG2	EC₅₀	1.6 μM Compound: Rosiglitazone	Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by PPAR-luciferase assay Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by PPAR-luciferase assay	[PMID: 25437304]
HepG2	EC₅₀	10 nM Compound: Rosiglitazone	Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay	[PMID: 21482446]
HepG2	EC₅₀	100 nM Compound: Rosiglitazone	Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay	[PMID: 22934537]
HepG2	EC₅₀	50 nM Compound: Rosiglitazone	Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay	[PMID: 21450468]
HepG2	EC₅₀	82 nM Compound: 1,rosiglitazone	Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay	[PMID: 17157019]
HepG2	EC₅₀	> 10 μM Compound: Rosiglitazone	Agonist activity at human PPAR alpha in HepG2 cells by PPAR-GAL4 transactivation assay Agonist activity at human PPAR alpha in HepG2 cells by PPAR-GAL4 transactivation assay	[PMID: 16979341]
HepG2	EC₅₀	> 10 μM Compound: rosiglitazone	Agonist activity at human PPAR alpha in a HepG2 cells by PPAR-GAL4 transactivation assay Agonist activity at human PPAR alpha in a HepG2 cells by PPAR-GAL4 transactivation assay	[PMID: 16973358]
HepG2	EC₅₀	> 12 μM Compound: 1, Rosi	Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay	[PMID: 18394907]
HepG2	EC₅₀	> 12 μM Compound: 3	Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay	[PMID: 19783444]
Hepatocyte	IC₅₀	165 μM Compound: Rosiglitazone	Cytotoxicity against rat primary hepatocytes after 16 hrs Cytotoxicity against rat primary hepatocytes after 16 hrs	10.1039/C3MD00377A
Hepatocyte	IC₅₀	225 μM Compound: Rosiglitazone	Cytotoxicity against rat primary hepatocytes after 6 hrs Cytotoxicity against rat primary hepatocytes after 6 hrs	10.1039/C3MD00377A
Huh-7	EC₅₀	0.22 μM Compound: 1	Functional activity at human PPAR gamma in Huh7 cells by transactivation assay Functional activity at human PPAR gamma in Huh7 cells by transactivation assay	[PMID: 16366601]
Huh-7	EC₅₀	0.22 μM Compound: 1	Effect on PPAR gamma transactivation activity in Huh7 cells Effect on PPAR gamma transactivation activity in Huh7 cells	[PMID: 16451087]
Huh-7	EC₅₀	0.22 μM Compound: rosiglitazone	Activity at human PPAR gamma in Huh7 cells by transactivation assay Activity at human PPAR gamma in Huh7 cells by transactivation assay	[PMID: 17034149]
Keratinocyte	IC₅₀	8 μM Compound: rosiglitazone	Antiproliferative activity against human keratinocytes Antiproliferative activity against human keratinocytes	[PMID: 16821769]
L6	EC₅₀	4.49 μM Compound: Rosiglitazone	Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose after 24 hrs in presence of insulin Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose after 24 hrs in presence of insulin	[PMID: 23992862]
L6	EC₅₀	5000 nM Compound: rosiglitazone	Effect on fatty acid oxidation in rat L6 cells Effect on fatty acid oxidation in rat L6 cells	[PMID: 17343371]
L6	IC₅₀	4.8 μM Compound: Rosi	Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells after 16 hrs by scintillation counting analysis Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells after 16 hrs by scintillation counting analysis	[PMID: 24813738]
MCF7	EC₅₀	87 nM Compound: rosiglitazone	Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay	[PMID: 26226490]
MCF7	IC₅₀	> 50 μM Compound: rosiglitazone	Antiproliferative activity against human MCF7 cell line Antiproliferative activity against human MCF7 cell line	[PMID: 16821769]
MDA-MB-231	IC₅₀	5.23 μM Compound: Rosiglitazone	Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 25278236]
MG-63	EC₅₀	11 nM Compound: Rosiglitazone	Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay	[PMID: 22225641]
MG-63	EC₅₀	11 nM Compound: Rosiglitazone	Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay	[PMID: 22727448]
NIH3T3	EC₅₀	0.32 μM Compound: Rosiglitazone	Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay	[PMID: 17624777]
NIH3T3	EC₅₀	0.32 μM Compound: rosiglitazone	Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay	[PMID: 16854085]
PC-3	IC₅₀	20.3 μM Compound: Rosiglitazone	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24996143]
Platelet	IC₅₀	5.7 mM Compound: 1; Rosi	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of ADP-induced platelet aggregation Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of ADP-induced platelet aggregation	[PMID: 30481687]
Platelet	IC₅₀	6.4 mM Compound: 1; Rosi	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of arachidonic acid-induced platelet aggregation Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of arachidonic acid-induced platelet aggregation	[PMID: 30481687]
RAW264.7	IC₅₀	17.5 μM Compound: BRL-49653	Suppression of LPS/IFN-gamma-stimulated NO production in mouse RAW264.7 cells Suppression of LPS/IFN-gamma-stimulated NO production in mouse RAW264.7 cells	[PMID: 18809325]
Sf21	IC₅₀	40 μM Compound: Rosiglitazone	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	6.4 μM Compound: Rosiglitazone	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
U2OS	EC₅₀	0.01 M Compound: Rosiglitazone	Agonist activity at human PPARgamma in human U2OS cells by cell based transactivation assay Agonist activity at human PPARgamma in human U2OS cells by cell based transactivation assay	[PMID: 19423341]
U2OS	EC₅₀	0.02 μM Compound: Rosiglitazone	Agonist activity at human PPARgamma in U2OS cells by transactivation assay Agonist activity at human PPARgamma in U2OS cells by transactivation assay	[PMID: 18329751]
U2OS	EC₅₀	0.03 μM Compound: rosiglitazone	Effect on PPARgamma transactivation activity in U2OS cells Effect on PPARgamma transactivation activity in U2OS cells	[PMID: 16300944]
U2OS	EC₅₀	0.05 μM Compound: rosiglitazone	Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay	[PMID: 19574056]
U2OS	EC₅₀	259.42 nM Compound: ROS	Transactivation of human PPARgamma transfected in U2OS cells co-tranfected with human RXR measured after 24 hrs by luciferase reporter assay Transactivation of human PPARgamma transfected in U2OS cells co-tranfected with human RXR measured after 24 hrs by luciferase reporter assay	[PMID: 31629632]
U2OS	IC₅₀	5.1 μM Compound: Rosiglitazone	Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method	[PMID: 31439379]

In Vitro

Rosiglitazone (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes^[1].
Rosiglitazone (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons^[3].
Rosiglitazone (1 μM, 24 h) protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner^[3].
Rosiglitazone (0.01-100 μM, 15 min) inhibits TRPM3 with IC₅₀ values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity respectively^[4].
Rosiglitazone (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation^[7].
Rosiglitazone (5 μM, 7 days) suppresses Olaparib (HY-10162) induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[7]

Cell Line:	A2780 and SKOV3 cells
Concentration:	0.5-50 μM
Incubation Time:	1-7 days
Result:	Inhibited cell proliferation in a time‑dependent and concentration‑dependent manner.

Western Blot Analysis^[3]

Cell Line:	Hippocampal neurons
Concentration:	1 μM
Incubation Time:	24 h
Result:	Increased NF-α1 and BCL-2 protein level.

In Vivo

Rosiglitazone (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats^[5].
Rosiglitazone (intraperitoneal injection, 3 mg/kg/day) ameliorates airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα in male Wistar rats^[6].
Rosiglitazone (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models^[7].
Rosiglitazone can exert neuroactive effects after intraperitoneal injection and modulate astrocyte polarization and neuroinflammation in a PPAR-γ dependent manner following experimental traumatic brain injury^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Streptozotocin (STZ)-induced diabetic rats^[5]
Dosage:	5 mg/kg
Administration:	Oral administration, daily for 8 weeks.
Result:	Decreased IL-6, TNF-α, and VCAM-1 levels in diabetic group. Displayed lower levels of lipid peroxidation and NOx with an increase in aortic GSH and SOD levels compared to diabetic groups.

Animal Model:	Male Wistar rats^[6]
Dosage:	3 mg/kg/day
Administration:	Intraperitoneal injection, twice a day, 6 days per week for 12 consecutive weeks
Result:	Ameliorated emphysema, elevated PEF, and higher level of total cells, neutrophils and cytokines (TNF-α and IL-1β) induced by cigarette smoke (CS). Inhibited CS-induced M1 macrophage polarization and decreased the ratio of M1/M2.

Essai clinique

Masse moléculaire

357.43

Formule

C₁₈H₁₉N₃O₃S

CAS No.

122320-73-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1)SC(CC2=CC=C(OCCN(C)C3=NC=CC=C3)C=C2)C1=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 175 mg/mL (489.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 2 mg/mL (5.60 mM; ultrasonic and warming and heat to 60°C)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7978 mL	13.9888 mL	27.9775 mL
5 mM	0.5596 mL	2.7978 mL	5.5955 mL
10 mM	0.2798 mL	1.3989 mL	2.7978 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (13.99 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (13.99 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (13.99 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (27.98 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.94%

Fiche technique (282 KB) SDS (393 KB)

COA (245 KB) HNMR (284 KB) RP-HPLC (218 KB) LCMS (94 KB) Elemental Analysis Report (103 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Lehmann JM, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995 Jun 2;270(22):12953-6. [Content Brief]

[2]. Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996 Feb 2;39(3):665-8. [Content Brief]

[3]. Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70. [Content Brief]

[4]. Majeed Y, et al. Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels. Mol Pharmacol. 2011 Jun;79(6):1023-30. [Content Brief]

[5]. Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96(3):215-220. [Content Brief]

[6]. Haoshen Feng, et al. Rosiglitazone ameliorated airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα. Int Immunopharmacol. 2021 Aug;97:107809. [Content Brief]

[7]. Zehua Wang, et al. Rosiglitazone ameliorates senescence and promotes apoptosis in ovarian cancer induced by olaparib. Cancer Chemother Pharmacol. 2020 Feb;85(2):273-284. [Content Brief]

[8]. Ren X, et al. Rosiglitazone regulates astrocyte polarization and neuroinflammation in a PPAR-γ dependent manner after experimental traumatic brain injury. Brain Res Bull. 2024 Apr;209:110918. [Content Brief]

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Référence

Description

Cond.

Prix HT

TFEH-PPARg-5

Human PPAR-gamma Activity Assay Kit

5PlateKit

TFEH-PPARg-1

Human PPAR-gamma Activity Assay Kit

1PlateKit

Rosiglitazone [122320-73-4]

Référence HY-17386-50mg

Marque : MedChemExpress

Rosiglitazone Related Antibodies

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