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BMS-986224
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产品介绍
产品介绍
产品信息
抗原名称
APJ receptor:0.3 nM (Kd), APJ receptor:0.02 nM (EC50, human)
简单描述
BMS-986224 是一种具有口服活性、有效性和选择性的 APJ 受体激动剂。BMS-986224 具有研究心力衰竭的潜力。
商品描述
BMS-986224 is an orally active, potent, and selective APJ receptor agonist. BMS-986224 has the potential to study heart failure.
分子量
498.92
纯度
99.67%
性状
Solid
颜色
Yellow
In vitro(体外研究)
Fully inhibits forskolin-mediated cAMP production, with an EC50 for human APJ of 0.02 nM, BMS-986224. 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.
In vivo(体内研究)
In the RHR model, BMS-986224 (0.192 mg/kg or 3 mg/kg; SC infusion; daily) increased stroke volume and cardiac output to levels seen in healthy animals, but without preventing cardiac hypertrophy and fibrosis. These effects are differentiated from enalapril[1].
背景
别名
BMS 986224
分子式
C24H23ClN4O6
CAS号
2055200-88-7
密度
1.366 g/cm3 (Predicted)
制备和贮存
溶解方法
DMSO: 10 mg/mL (20.04 mM), Sonication is recommended.
存储溶液
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
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