YL-GB063
YL-GB063 is an Apelin receptor (APJ) antagonist. YL-GB063 inhibits Apelin-induced APJ β-arrestin recruitment (IC50 of 3.1 μM in HTLA cells). YL-GB063 has anti-cancer activity against ovarian cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C17H12ClN3O6S2
- Masse moléculaire:453.88
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
In Vitro
YL-GB063 (30 min) potently inhibits Apelin-induced APJ β-arrestin recruitment in transiently transfected HTLA cells, with an IC50 of 3.1 μM[1].
The half-lives of YL-GB063 in mouse liver microsomes is 14.1 min[1].
YL-GB063 (12.5-50 μM; 3 days) inhibits the viability of OVCAR8 ovarian cancer cells[1].
YL-GB063 (30 μM; 8 h) completely inhibits Apelin-induced migration of APJ-transfected HUVEC-APJ endothelial cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:OVCAR8 ovarian cancer cells
-
Concentration:12.5, 25, 50 μM
-
Incubation Time:3 days (daily treatment)
-
Result:Inhibited OVCAR8 cell viability with an IC50 of 23.2 μM and achieved 96.0% maximal inhibition.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:athymic nude mice (female, 6−8 weeks old)[1]
-
Dosage:100 mg/kg
-
Administration:i.p.; daily
-
Result:Prolonged median survival time to 43 days (control: 30 days).
Reduced abdominal circumferences significantly by day 21 compared to control and ML221 groups.
Decreased metastatic tumor nodule count compared to control group.
Reduced ascites incidence to 4 of 7 mice (control: all mice).
Chemical Information
-
Masse moléculaire 453.88
-
Formule C17H12ClN3O6S2
-
SMILES
[O-][N+](C1=CC=C(C=C1)S(OC2=CC=C(C=C2O)CSC3=NC=C(C=N3)Cl)(=O)=O)=O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YL-GB063 Related Classifications
HY-181540 Related Classifications
Powered by Bioz