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BMS-986224
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-986224图片
CAS NO:2055200-88-7
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
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。
Cas No.2055200-88-7
分子式C24H23ClN4O6
分子量498.92
溶解度DMSO : 20.83 mg/mL (41.75 mM; ultrasonic and warming and heat to 60°C)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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[1].

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].

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].

[1]. Gargalovic P, et al. In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure. Circ Heart Fail. 2021;14(3):e007351.