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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- 화학식: C17H12ClN3O6S2
- 분자량:453.88
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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.
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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.
In Vivo
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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분자량 453.88
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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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.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YL-GB063 Related Classifications
HY-181540 Related Classifications
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