Rutaecarpine [84-26-4]

Katalog-Nummer HY-N0147-10mg

Size : 10mg

Marke : MedChemExpress


Beschreibung

Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB).

IC50 & Target[1]

COX-2

0.28 μM (IC50, in BMMC)

COX-1

8.7 μM (IC50, in BMMC)

Cellular Effect
Cell Line Type Value Description References
A549 GI50
14.5 μM
Compound: 11a
Tested for in vitro cytotoxicity against non-small cell lung cancer cell line A549/ATCC
Tested for in vitro cytotoxicity against non-small cell lung cancer cell line A549/ATCC
10.1016/0960-894X(95)00046-V
A549 GI50
14.5 μM
Compound: 49
Growth inhibition of human A549 cells by SRB assay
Growth inhibition of human A549 cells by SRB assay
[PMID: 36375335]
A549 IC50
> 20 μM
Compound: Fig 1A, Cpd 1
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 38897138]
CCD-18Co IC50
> 50 μM
Compound: 1
Antiproliferative activity against human CCD-18Co cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
Antiproliferative activity against human CCD-18Co cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
[PMID: 35544614]
CCD-841CoN IC50
> 50 μM
Compound: 1
Antiproliferative activity against human CCD-841CoN cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
Antiproliferative activity against human CCD-841CoN cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
[PMID: 35544614]
CCRF-CEM GI50
18.9 μM
Compound: 11a
Tested for in vitro cytotoxicity against leukemia cell line CCRF-CEM
Tested for in vitro cytotoxicity against leukemia cell line CCRF-CEM
10.1016/0960-894X(95)00046-V
DU-145 GI50
31.65 μM
Compound: 49
Growth inhibition of human DU-145 cells incubated for 48 hrs by sulforhodamine B assay
Growth inhibition of human DU-145 cells incubated for 48 hrs by sulforhodamine B assay
[PMID: 36375335]
HCT-116 GI50
33.89 μM
Compound: 49
Anticancer activity against human HCT-116 cells assessed as cell growth inhibition
Anticancer activity against human HCT-116 cells assessed as cell growth inhibition
[PMID: 36375335]
HCT-116 IC50
31.1 μM
Compound: 1
Antiproliferative activity against human HCT-116 cells harboring beta-catenin mutant assessed as reduction in cell viability measured after 72 hrs by SRB assay
Antiproliferative activity against human HCT-116 cells harboring beta-catenin mutant assessed as reduction in cell viability measured after 72 hrs by SRB assay
[PMID: 35544614]
HCT-15 IC50
> 50 μM
Compound: 1
Antiproliferative activity against human HCT-15 cells harboring wild type beta-catenin assessed as reduction in cell viability measured after 72 hrs by SRB assay
Antiproliferative activity against human HCT-15 cells harboring wild type beta-catenin assessed as reduction in cell viability measured after 72 hrs by SRB assay
[PMID: 35544614]
HEK293 EC50
2.06 μM
Compound: 2
Agonist activity at rat TRPV1 channel expressed in HEK293 cells assessed as induction of channel current at -60 mV holding potential by whole-cell patch-clamp method
Agonist activity at rat TRPV1 channel expressed in HEK293 cells assessed as induction of channel current at -60 mV holding potential by whole-cell patch-clamp method
[PMID: 27159637]
HL-60 GI50
19.8 μM
Compound: 49
Growth inhibition of human HL-60 cells incubated for 4 days by WST assay
Growth inhibition of human HL-60 cells incubated for 4 days by WST assay
[PMID: 36375335]
HT-29 GI50
31.6 μM
Compound: 49
Growth inhibition of human HT-29 cells by SRB assay
Growth inhibition of human HT-29 cells by SRB assay
[PMID: 36375335]
HT-29 IC50
118 μM
Compound: 49
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by SRB assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by SRB assay
[PMID: 36375335]
HUVEC IC50
16.54 μM
Compound: 49
Cytotoxicity against HUVEC cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against HUVEC cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 36375335]
HeLa EC50
26.1 μM
Compound: 1a
Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
[PMID: 28958621]
HeLa IC50
26 μM
Compound: Fig 1A, Cpd 1
Antiproliferative activity against human HeLa cells
Antiproliferative activity against human HeLa cells
[PMID: 38897138]
Hs-578T GI50
22.6 μM
Compound: 11a
Tested for in vitro cytotoxicity against breast cancer cell line Hs 578.T
Tested for in vitro cytotoxicity against breast cancer cell line Hs 578.T
10.1016/0960-894X(95)00046-V
Hs-578T GI50
22.6 μM
Compound: 49
Growth inhibition against human Hs-578T cells incubated for 48 hrs by sulforhodamine B reagent assay
Growth inhibition against human Hs-578T cells incubated for 48 hrs by sulforhodamine B reagent assay
[PMID: 36375335]
K562 GI50
25.77 μM
Compound: 49
Growth inhibition of human K562 cells incubated for 48 hrs by sulforhodamine B assay
Growth inhibition of human K562 cells incubated for 48 hrs by sulforhodamine B assay
[PMID: 36375335]
LS174T IC50
6.1 μM
Compound: 1
Antiproliferative activity against human LS174T cells harboring beta-catenin mutant assessed as reduction in cell viability measured after 72 hrs by SRB assay
Antiproliferative activity against human LS174T cells harboring beta-catenin mutant assessed as reduction in cell viability measured after 72 hrs by SRB assay
[PMID: 35544614]
MCF-10A IC50
> 20 μM
Compound: Fig 1A, Cpd 1
Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 38897138]
MCF7 GI50
19.57 μM
Compound: 49
Growth inhibition of human MCF7 cells incubated for 48 hrs by SRB assay
Growth inhibition of human MCF7 cells incubated for 48 hrs by SRB assay
[PMID: 36375335]
MCF7 IC50
74.5 μM
Compound: 49
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 36375335]
MCF7 IC50
> 20 μM
Compound: Fig 1A, Cpd 1
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 38897138]
MDA-MB-231 IC50
117.6 μM
Compound: 49
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by SRB assay
[PMID: 36375335]
NCI-N87 GI50
8.41 μM
Compound: 49
Growth inhibition of human NCI-N87 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Growth inhibition of human NCI-N87 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 36375335]
OVCAR-4 GI50
18.9 μM
Compound: 11a
Tested for in vitro cytotoxicity against ovarian cancer cell line OVCAR-4
Tested for in vitro cytotoxicity against ovarian cancer cell line OVCAR-4
10.1016/0960-894X(95)00046-V
OVCAR-4 GI50
18.9 μM
Compound: 49
Growth inhibition of human OVCAR-4 cells by SRB assay
Growth inhibition of human OVCAR-4 cells by SRB assay
[PMID: 36375335]
P388 IC50
36.8 μM
Compound: 49
Cytotoxicity against mouse P388 cells assessed as inhibition of cell growth incubated for 48 hrs by SRB assay
Cytotoxicity against mouse P388 cells assessed as inhibition of cell growth incubated for 48 hrs by SRB assay
[PMID: 36375335]
RKO IC50
> 50 μM
Compound: 1
Antiproliferative activity against human RKO cells harboring wild type beta-catenin assessed as reduction in cell viability measured after 72 hrs by SRB assay
Antiproliferative activity against human RKO cells harboring wild type beta-catenin assessed as reduction in cell viability measured after 72 hrs by SRB assay
[PMID: 35544614]
SF-295 GI50
14.1 μM
Compound: 49
Growth inhibition against human SF-295 cells incubated for 48 hrs by sulforhodamine B assay
Growth inhibition against human SF-295 cells incubated for 48 hrs by sulforhodamine B assay
[PMID: 36375335]
SMMC-7721 IC50
18.9 μM
Compound: 49
Anticancer activity against human SMMC-7721 cells assessed as cell growth inhibition incubated for 48 hrs by CCK8 assay
Anticancer activity against human SMMC-7721 cells assessed as cell growth inhibition incubated for 48 hrs by CCK8 assay
[PMID: 36375335]
SW480 IC50
> 50 μM
Compound: 1
Antiproliferative activity against human SW480 cells harboring wild type beta-catenin assessed as reduction in cell viability measured after 72 hrs by SRB assay
Antiproliferative activity against human SW480 cells harboring wild type beta-catenin assessed as reduction in cell viability measured after 72 hrs by SRB assay
[PMID: 35544614]
U-251 GI50
0.02 μM
Compound: 49
Growth inhibition of human U-251 cells by sulforhodamine B assay
Growth inhibition of human U-251 cells by sulforhodamine B assay
[PMID: 36375335]
In Vitro

Rutaecarpine has shown a variety of intriguing biological properties such as anti-thrombotic, anticancer, anti-inflammatory and analgesic, anti-obesity and thermoregulatory, vasorelaxing activity, as well as effects on the cardiovascular and endocrine systems[2]. Rutaecarpine inhibits COX-2 and COX-1 dependent phases of PGD2 generation in BMMC in a concentration-dependent manner with an IC50 of 0.28 μM and 8.7 μM, respectively. It inhibits COX-2-dependent conversion of exogenous arachidonic acid to PGE2 in a dose-dependent manner by the COX-2-transfected HEK293 cells[1].

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

In Vivo

Rutaecarpine showed in vivo anti-inflammatory activity on rat l-carrageenan induced paw edema by intraperitoneal administration[1]. Rutaecarpine significantly decreases the number of antibody-forming cells and causes weight decrease in spleen in a dose-dependent manner. In addition, rutaecarpine administered mice exhibit reduced splenic cellularity, decreased numbers of total T cells, CD4+ cells, CD8+ cells, and B cells in spleen. IL-2, interferon and IL-10 mRNA expressions are suppressed significantly by rutaecarpine treatment. The number of CD4+IL-2+ cells is reduced significantly following administration of mice with rutaecarpine[3].

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

Molekulargewicht

287.32

Formel

C18H13N3O

CAS. Nr.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N2C(C(NC3=C4C=CC=C3)=C4CC2)=NC5=C1C=CC=C5

Structure Classification
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 50 mg/mL (174.02 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 3.4804 mL 17.4022 mL 34.8044 mL
5 mM 0.6961 mL 3.4804 mL 6.9609 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation
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