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BMS-986224 

Cat. No.: HY-139485
Handling Instructions

BMS-986224 is a potent, selective and orally bioavailable APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr1) apelin-13. BMS-986224 has the potential for the research of heart failure.

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

BMS-986224 Chemical Structure

BMS-986224 Chemical Structure

CAS No. : 2055200-88-7

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Description

BMS-986224 is a potent, selective and orally bioavailable APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr1) apelin-13. BMS-986224 has the potential for the research of heart failure[1].

IC50 & Target

Kd: 0.3 nM (APJ receptor)

In Vitro

BMS-986224 fully inhibits forskolin-mediated cAMP production, with an EC50 for human APJ of 0.02 nM. BMS-986224 (0-100 nM) fully stimulates β-arrestin recruitment, ERK phosphorylation, and APJ internalization in Chinese hamster ovary-K1 or HEK293 ZF cells[1].
BMS-986224 is a potent and selective APJ receptor agonist that exhibits a similar signaling profile to (Pyr1) apelin-13[1].

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

In Vivo

BMS-986224 (0.192 mg/kg or 3 mg/kg; SC infusion; daily;) in the RHR model increased stroke volume and cardiac output to levels seen in healthy animals but without preventing cardiac hypertrophy and fibrosis, effects differentiated from enalapril[1].

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

Animal Model: Male Sprague-Dawley rats (renal hypertensive rat model)[1]
Dosage: 0.192 mg/kg or 3 mg/kg
Administration: SC infusion; daily; Initiated 3 days before surgery and continued for 7 days after surgery
Result: The achieved steady-state plasma concentrations during 10-day infusion were 102 and 2686 nmol/L at low dose and HD, respectively. At the low dose, BMS-986224 increased SV and CO without affecting other measured parameters, including the measured diastolic parameters, cardiac fibrosis, and heart weight in RHR.
Clinical Trial
Molecular Weight

498.92

Formula

C₂₄H₂₃ClN₄O₆

CAS No.
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Storage

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

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BMS-986224
Cat. No.:
HY-139485
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