2. GPCR/G Protein
  3. Apelin Receptor (APJ)
  4. 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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YL-GB063

YL-GB063 Chemical Structure

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YL-GB063 Related Antibodies

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Description

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[1].

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.

YL-GB063 Related Antibodies

Cell Viability Assay[1]

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

YL-GB063 (100 mg/kg; i.p.; daily) significantly extends the median survival time to 43 days, reduces ascites formation and disease progression in a mouse model of orthotopic ovarian cancer xenografts[1].

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).
Molecular Weight

453.88

Formula

C17H12ClN3O6S2
SMILES

[O-][N+](C1=CC=C(C=C1)S(OC2=CC=C(C=C2O)CSC3=NC=C(C=N3)Cl)(=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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YL-GB063 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YL-GB063Apelin Receptor (APJ)apelin receptorOVCAR8 ovarian cancer cellsOVCAR3 ovarian cancer cellsAPJOVCAR8-APJ ovarian cancer cellsOVCAR8-EV cellsβ-arrestinHTLA cellsorthotopic ovarian cancer xenograft mouse modelHUVEC-APJ endothelial cellsInhibitorinhibitorinhibit

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