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Cat. No.: HY-181540

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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.

For research use only. We do not sell to patients.

Formula: C₁₇H₁₂ClN₃O₆S₂
Molecular Weight:453.88

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

YL-GB063 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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.

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).

Chemical Information

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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Elsheikh A, et al. Design, Synthesis, and Pharmacological Evaluation of Metabolically Stable Apelin Receptor Antagonists with Improved In Vivo Exposure and Efficacy in Ovarian Cancer. J Med Chem. 2026;69(3):3404-3423. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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