Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

Rapamycin [53123-88-9]

Stampa

Cat# HY-10219-100mg

Size : 100mg

Marca : MedChemExpress

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Description

Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant^[1]^[2]^[3]^[4]^[5].

IC₅₀ & Target^[1]^[2]

mTOR

0.1 nM (IC₅₀, in HEK293 cells )

Microbial Metabolite

FKBP12

Autophagy

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	18.74 μM Compound: Rapamycin	Antiproliferative activity against human A549 cells by MTT assay Antiproliferative activity against human A549 cells by MTT assay	[PMID: 31546197]
A549	IC₅₀	30.72 μM Compound: Rapamycin	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33862514]
A549	IC₅₀	49.35 μM Compound: Rapamycin	Antitumor activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer-Glo assay Antitumor activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer-Glo assay	[PMID: 35688004]
C-33-A	IC₅₀	<50 nM Compound: 25	Antiproliferative activity against human C-33-A cells assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay Antiproliferative activity against human C-33-A cells assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay	[PMID: 36669398]
Caov-3 cell line	IC₅₀	<50 nM Compound: 25	Antiproliferative activity against human Caov-3 cell line assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay Antiproliferative activity against human Caov-3 cell line assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay	[PMID: 36669398]
DU-145	IC₅₀	4 μM Compound: Rapamycin	Antitumor activity against human DU-145 cells assessed as cell growth inhibition Antitumor activity against human DU-145 cells assessed as cell growth inhibition	[PMID: 35688004]
HCT-8	IC₅₀	1.25 μM Compound: Sirolimus	TP_TRANSPORTER: inhibition of Rhodamine 123 transport (basal to apical) (R123: 15 uM) in HCT-8 cells TP_TRANSPORTER: inhibition of Rhodamine 123 transport (basal to apical) (R123: 15 uM) in HCT-8 cells	[PMID: 12235265]
HEK293	IC₅₀	1.1 μM Compound: Rapamycin	TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells	[PMID: 14530907]
HEK293	IC₅₀	0.1 nM Compound: rapamycin	Inhibition of mTOR kinase expressed in human HEK293 cells by Western blot analysis Inhibition of mTOR kinase expressed in human HEK293 cells by Western blot analysis	[PMID: 17350953]
HEK293	EC₅₀	0.05 μM Compound: Rapamycin	Inhibition of TPA-induced degradation of Pdcd4 (amino acid 39-91) expressed in human HEK293 cells assessed as minimum compound concentration required for 50% recovery of Pdcd4-luciferase signal incubated for 8 hrs by luciferase reporter gene assay Inhibition of TPA-induced degradation of Pdcd4 (amino acid 39-91) expressed in human HEK293 cells assessed as minimum compound concentration required for 50% recovery of Pdcd4-luciferase signal incubated for 8 hrs by luciferase reporter gene assay	[PMID: 21539301]
HEK293	IC₅₀	0.1 nM Compound: Rapamycin	Inhibition of mTOR in HEK293 cells Inhibition of mTOR in HEK293 cells	[PMID: 32324396]
HEK-293T	EC₅₀	0.1 nM Compound: RAPA	Antiviral activity against HIV1 R5 assessed as inhibition of cell-cell fusion between R5-envelope expressing HEK293T cells and CD8 depleted human PBMCs pretreated for 6 days Antiviral activity against HIV1 R5 assessed as inhibition of cell-cell fusion between R5-envelope expressing HEK293T cells and CD8 depleted human PBMCs pretreated for 6 days	[PMID: 17485501]
HEK-293T	EC₅₀	1.3 nM Compound: RAPA	Antiviral activity against HIV1 X4 assessed as inhibition of cell-cell fusion between X4-envelope expressing HEK293T cells and CD8 depleted human PBMCs pretreated for 6 days Antiviral activity against HIV1 X4 assessed as inhibition of cell-cell fusion between X4-envelope expressing HEK293T cells and CD8 depleted human PBMCs pretreated for 6 days	[PMID: 17485501]
HeLa	IC₅₀	>10000 nM Compound: Rapamycin	Growth inhibition of human HeLa cells after 72 hrs by CCK8 assay Growth inhibition of human HeLa cells after 72 hrs by CCK8 assay	[PMID: 29308895]
HeLa	IC₅₀	0.77 μM Compound: Rapamycin	Cytotoxicity against human HeLa cells Cytotoxicity against human HeLa cells	[PMID: 30015070]
HepG2	EC₅₀	10 μM Compound: Sirolimus	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis	[PMID: 20966043]
HepG2	CC₅₀	67.2 μM Compound: 78	Cytotoxicity against human HepG2 assessed as reduction in cell viability after 24 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human HepG2 assessed as reduction in cell viability after 24 hrs by CellTiter-Glo luminescent assay	[PMID: 28051303]
HT-3	IC₅₀	<50 nM Compound: 25	Antiproliferative activity against human HT-3 cells assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay Antiproliferative activity against human HT-3 cells assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay	[PMID: 36669398]
K562	IC₅₀	1 mM Compound: rapamycin	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 18571290]
MCF7	IC₅₀	4980 nM Compound: Rapamycin	Growth inhibition of human MCF7 cells after 72 hrs by CCK8 assay Growth inhibition of human MCF7 cells after 72 hrs by CCK8 assay	[PMID: 29308895]
MCF7	IC₅₀	18.74 μM Compound: Rapamycin	Antiproliferative activity against human MCF7 cells by MTT assay Antiproliferative activity against human MCF7 cells by MTT assay	[PMID: 31546197]
MCF7	EC₅₀	<1 nM Compound: Rapamycin	Cytotoxicity against human MCF7 cells after 5 days by Presto blue reagent-based fluorescence analysis Cytotoxicity against human MCF7 cells after 5 days by Presto blue reagent-based fluorescence analysis	10.1039/C5MD00493D
MDA-MB-231	IC₅₀	>10000 nM Compound: Rapamycin	Growth inhibition of human MDA-MB-231 cells after 72 hrs by CCK8 assay Growth inhibition of human MDA-MB-231 cells after 72 hrs by CCK8 assay	[PMID: 29308895]
MDA-MB-231	GI₅₀	>100 nM Compound: Rapamycin	Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 32510949]
MDA-MB-231	IC₅₀	0.9 μM Compound: Rapamycin	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	IC₅₀	35.79 μM Compound: Rapamycin	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33862514]
MDA-MB-453	GI₅₀	0.05 nM Compound: Rapamycin	Antiproliferative activity against human MDA-MB-453 cells incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human MDA-MB-453 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 32510949]
MDA-MB-468	IC₅₀	37.2 μM Compound: Rapamycin	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33862514]
ME-180	IC₅₀	<50 nM Compound: 25	Antiproliferative activity against human ME-180 cells assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay Antiproliferative activity against human ME-180 cells assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay	[PMID: 36669398]
MEF	IC₅₀	0.05 nM Compound: Sirolimus	Inhibition of mTOR in mouse TSC1-/- MEF cells assessed as inhibition of S6 Ser240/244 phosphorylation incubated for 2 hrs by fluorescence based assay Inhibition of mTOR in mouse TSC1-/- MEF cells assessed as inhibition of S6 Ser240/244 phosphorylation incubated for 2 hrs by fluorescence based assay	[PMID: 31223435]
MV4-11	IC₅₀	>500 nM Compound: RAPA	Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay	[PMID: 30629434]
NCI-H460	IC₅₀	>10000 nM Compound: Rapamycin	Growth inhibition of human H460 cells after 72 hrs by CCK8 assay Growth inhibition of human H460 cells after 72 hrs by CCK8 assay	[PMID: 29308895]
OCI-AML2	IC₅₀	>500 nM Compound: RAPA	Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay	[PMID: 30629434]
OCI-AML-3	IC₅₀	>500 nM Compound: RAPA	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay	[PMID: 30629434]
OVCAR-5	IC₅₀	>10000 nM Compound: Rapamycin	Growth inhibition of human OVCAR5 cells after 72 hrs by CCK8 assay Growth inhibition of human OVCAR5 cells after 72 hrs by CCK8 assay	[PMID: 29308895]
OVCAR-8	IC₅₀	<50 nM Compound: 25	Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay	[PMID: 36669398]
PC-3	IC₅₀	<0.01 μM Compound: Rapamycin	Antiproliferative activity against human PC3 cells Antiproliferative activity against human PC3 cells	[PMID: 21978683]
PC-3	IC₅₀	<0.01 μM Compound: Rapamycin	Inhibition of mTOR-mediated S6 phosphorylation in human PC3 cells Inhibition of mTOR-mediated S6 phosphorylation in human PC3 cells	[PMID: 21978683]
PC-3	IC₅₀	>10 μM Compound: Rapamycin	Inhibition of mTOR-mediated Akt phosphorylation in human PC3 cells Inhibition of mTOR-mediated Akt phosphorylation in human PC3 cells	[PMID: 21978683]
PC-3	EC₅₀	43.1 μM Compound: Rapamycin	Cytotoxicity against human PC3 cells by MTT assay Cytotoxicity against human PC3 cells by MTT assay	[PMID: 28774426]
PC-3	IC₅₀	1.3 μM Compound: Rapamycin	Antitumor activity against human PC-3 cells assessed as cell growth inhibition Antitumor activity against human PC-3 cells assessed as cell growth inhibition	[PMID: 35688004]
SF-268	IC₅₀	2.7 μM Compound: Rapamycin	Antitumor activity against human SF-268 cells assessed as cell growth inhibition Antitumor activity against human SF-268 cells assessed as cell growth inhibition	[PMID: 35688004]
SiHa	IC₅₀	1756 nM Compound: Rapamycin	Growth inhibition of human SiHa cells after 72 hrs by CCK8 assay Growth inhibition of human SiHa cells after 72 hrs by CCK8 assay	[PMID: 29308895]
SK-MEL-2	IC₅₀	1 μM Compound: Rapamycin	Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of LY3214996 by MTT assay Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of LY3214996 by MTT assay	[PMID: 36961300]
SK-MEL-2	IC₅₀	1 μM Compound: Rapamycin	Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of MEK-162 by MTT assay Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of MEK-162 by MTT assay	[PMID: 36961300]
SK-OV-3	IC₅₀	>10000 nM Compound: Rapamycin	Growth inhibition of human SKOV3 cells after 72 hrs by CCK8 assay Growth inhibition of human SKOV3 cells after 72 hrs by CCK8 assay	[PMID: 29308895]
SK-OV-3	IC₅₀	<50 nM Compound: 25	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 5 to 7 days by MTS assay	[PMID: 36669398]
SUM185PE	GI₅₀	0.04 nM Compound: Rapamycin	Antiproliferative activity against human SUM185PE cells incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human SUM185PE cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 32510949]
T47D	IC₅₀	1576 nM Compound: Rapamycin	Growth inhibition of human T47D cells after 72 hrs by CCK8 assay Growth inhibition of human T47D cells after 72 hrs by CCK8 assay	[PMID: 29308895]
T-cell	IC₅₀	1.6 nM Compound: 1	T-cell antiproliferative activity in human mixed lymphocyte reaction T-cell antiproliferative activity in human mixed lymphocyte reaction	[PMID: 16185865]
T-cell	IC₅₀	2600 nM Compound: 1	Antiproliferative activity in Lewis rat lymph node cells in rat mixed lymphocyte reaction Antiproliferative activity in Lewis rat lymph node cells in rat mixed lymphocyte reaction	[PMID: 16185865]
T-cell	IC₅₀	9.8 nM Compound: 1	Tested for inhibition of T cell proliferation in the co-mitogen stimulated proliferation assay Tested for inhibition of T cell proliferation in the co-mitogen stimulated proliferation assay	10.1016/0960-894X(95)00223-G
U-87MG ATCC	IC₅₀	10 μM Compound: Rapamycin	Antitumor activity against human U-87 MG cells assessed as cell growth inhibition Antitumor activity against human U-87 MG cells assessed as cell growth inhibition	[PMID: 35688004]

In Vitro

Rapamycin (12.5-100 nM; 24 hours) treatment exerts modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines (A549, SPC-A-1, 95D and NCI-H446 cells) tested, achieving about 30-40% reduction in cell proliferation at 100 nM vs. ~10% reduction at 12.5 nM^[3].
Lung cancer cell line 95D cells are exposed to Rapamycin (10 nM, 20 nM) and RP-56976 (1 nM, 10 nM) alone or in combination (Rapamycin 20 nM+ RP-56976 10 nM). After 24 hours exposure to Rapamycin or RP-56976 alone does not significantly alter the level of expression or phosphorylation of ERK1/2, whereas cells treated with the combination of Rapamycin with RP-56976 exhibit a marked reduction in the phosphorylation levels of ERK1/2^[3].

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

Cell Viability Assay^[3]

Cell Line:	Lung cancer cell lines A549, SPC-A-1, 95D and NCI-H446
Concentration:	12.5 nM, 25 nM, 50 nM, 100 nM
Incubation Time:	24 hours
Result:	Treatment exerted modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines.

Western Blot Analysis^[3]

Cell Line:	95D cells
Concentration:	10 nM and 20 nM
Incubation Time:	24 hours
Result:	Combination treatment with RP-56976 decreased phosphorylation of ERK.

In Vivo

Rapamycin (2.0 mg/kg; intraperitoneal injection; every other day; 28 days) alone has a moderate inhibitory effect. However, the combination of Metformin (HY-B0627) and Rapamycin exerts a significantly increased inhibition of tumor growth compared with the control group, the Rapamycin monotherapy group and the Metformin monotherapy group^[4].

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

Animal Model:	24 male nu/nu mice aged 4-5 week old (15-20 g)^[4]
Dosage:	2.0 mg/kg
Administration:	Intraperitoneal injection; every other day; 28 days
Result:	Had a moderate inhibitory effect in monotherapy group. The combination with Metformin exerted a significantly increased inhibition of tumor growth.

Essai clinique

Masse moléculaire

914.17

Formule

C₅₁H₇₉NO₁₃

CAS No.

53123-88-9

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@]1(O)[C@@H](CC[C@@H](C[C@@H](/C(C)=C/C=C/C=C/[C@H](C[C@@H](C)C([C@@H]([C@@H](/C(C)=C/[C@H]2C)O)OC)=O)C)OC)O1)C)C(N3CCCC[C@H]3C(O[C@@H](CC2=O)[C@@H](C[C@H]4C[C@H]([C@H](O)CC4)OC)C)=O)=O

Structure Classification

Initial Source

Microorganisms

bacterium Streptomyces hygroscopicus

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 : 100 mg/mL (109.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0939 mL	5.4694 mL	10.9389 mL
5 mM	0.2188 mL	1.0939 mL	2.1878 mL
10 mM	0.1094 mL	0.5469 mL	1.0939 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: ≥ 2.5 mg/mL (2.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (2.73 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (2.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.94%

Fiche technique (286 KB) SDS (396 KB)

COA (259 KB) HNMR (241 KB) LCMS (121 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Edwards SR, et al. The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. J Biol Chem, 2007, 282(18), 13395-13401. [Content Brief]

[2]. Rangaraju S, et al. Rapamycin activates autophagy and improves myelination in explant cultures from neuropathicmice. J Neurosci. 2010 Aug 25;30(34):11388-97. [Content Brief]

[3]. Niu H, et al. Rapamycin potentiates cytotoxicity by RP-56976 possibly through downregulation of Survivin in lung cancer cells. J Exp Clin Cancer Res. 2011 Mar 10;30:28. [Content Brief]

[4]. Zhang JW, et al. Metformin synergizes with rapamycin to inhibit the growth of pancreatic cancer in vitro and in vivo. Oncol Lett. 2018 Feb;15(2):1811-1816. [Content Brief]

[5]. Svensson JE, et al. Evaluating the effect of rapamycin treatment in Alzheimer's disease and aging using in vivo imaging: the ERAP phase IIa clinical study protocol. BMC Neurol. 2024 Apr 4;24(1):111. [Content Brief]

[6]. Soini L, et al. Molecular glues to stabilise protein-protein interactions. Curr Opin Chem Biol. 2022 Aug;69:102169. [Content Brief]

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Rapamycin [53123-88-9]

Cat# HY-10219-100mg

Marca : MedChemExpress

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