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.
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- Formule: C17H12ClN3O6S2
- Masse moléculaire:453.88
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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Cell Line:OVCAR8 ovarian cancer cells
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Concentration:12.5, 25, 50 μM
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Incubation Time:3 days (daily treatment)
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Result:Inhibited OVCAR8 cell viability with an IC50 of 23.2 μM and achieved 96.0% maximal inhibition.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic nude mice (female, 6−8 weeks old)[1]
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Dosage:100 mg/kg
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Administration:i.p.; daily
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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
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Masse moléculaire 453.88
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Formule C17H12ClN3O6S2
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SMILES
[O-][N+](C1=CC=C(C=C1)S(OC2=CC=C(C=C2O)CSC3=NC=C(C=N3)Cl)(=O)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YL-GB063 Related Classifications
HY-181540 Related Classifications
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