BMS-986224

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMS-986224 是一种有效选择性和具有口服活性的 APJ 受体激动剂 (Kd = 0.3 nM)，表现出与 (Pyr1) apelin-13 相似的受体结合和信号传导谱。BMS-986224 具有研究心力衰竭的潜力。

BMS-986224 is a potent, selective and orally active 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.

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.BMS-986224 is a potent and selective APJ receptor agonist that exhibits a similar signaling profile to (Pyr1) apelin-13.

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.Animal Model:Male Sprague-Dawley rats (renal hypertensive rat model)Dosage:0.192 mg/kg or 3 mg/kgA dministration: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.

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Others

Other Targets

Apelin receptor

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2055200-88-7

498.92

C24H23ClN4O6

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 20.83 mg/mL (41.75 mM; 超声助溶 (<60°C)

CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cn3)o2)c(O)c1-c1c(OC)cccc1OC

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(-20℃)

With Ice Pack

≥ 2 years