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Cat. No.: HY-175818

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APJ antagonist-1

APJ antagonist-1 is an apelin receptor (APJ) antagonist. APJ antagonist-1 shows strong β-arrestin inhibition with an IC₅₀ of 3.1 μM. APJ antagonist-1 selectively inhibits APJ-overexpressing cancer cells and suppresses apelin-induced endothelial cell migration. APJ antagonist-1exhibits high metabolic stability. APJ antagonist-1 can used for the studies of ovarian cancer and tumor angiogenesis.

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

Formula: C₁₈H₁₅N₃O₆S₂
Molecular Weight:433.46

Storage:

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

Data Sheet (273 KB)

APJ antagonist-1 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
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

In Vitro

APJ antagonist-1 (Compound 21) (1 h) exhibits significantly enhanced metabolic stability than ML221 (HY-103254) (100 % remaining in plasma after 1 h; liver microsomal t_1/2 = 5 min)^[1].
APJ antagonist-1 (12.5-100 μM, 3 days) shows a greater reduction in the viability of OVCAR8 cells and HT-29 cells^[1].
APJ antagonist-1 (30 μM, 8 h) significantly inhibits Apelin (HY-175818)-induced migration in OVCAR3 cells and HUVECs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Migration Assay ^[1]

Cell Line:

OVCAR3 cells and HUVECs
Concentration:

30 μM
Incubation Time:

8 h
Result:

Significantly inhibited apelin-induced migration and the effect was comparable to or even better than ML211.

Chemical Information

Molecular Weight 433.46
Formula C₁₈H₁₅N₃O₆S₂
SMILES

O=S(C1=CC=C([N+]([O-])=O)C=C1)(OC2=CC(CSC3=NC=CC=N3)=CC=C2OC)=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 (273 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]. Bist G, et al. Novel small molecule analogs for advancing apelin receptor antagonism with enhanced plasma and microsomal stability. Bioorg Med Chem Lett. 2025 Aug 8;129:130367. [Content Brief]

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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.

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100 mg

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