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首页-小分子抑制剂&激动剂-GPCR-Apelin Receptor (APLNR)-BMS-986224
BMS-986224

Chemical Structure : BMS-986224

CAS No.: 2055200-88-7

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BMS-986224 (BMS986224)

货号: PC-38138Not For Human Use, Lab Use Only.

BMS-986224 (BMS986224) is a novel potent, selective, orally bioavailable agonist of Apelin receptor (APJ, APLNR) with Ki of 0.074 nM (human APJ).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BMS-986224 (BMS986224) is a novel potent, selective, orally bioavailable agonist of Apelin receptor (APJ, APLNR) with Ki of 0.074 nM (human APJ).
BMS-986224 is highly selective for the APJ receptor and did not bind other GPCRs at 30 uM concentration.
BMS-986224 showed to be a fully competitive and high-affinity orthosteric ligand, displacing (Pyr1) apelin-13 from the human APJ receptor.
BMS-986224 inhibited forskolin-mediated cAMP production (EC50=0.02 nM), stimulate β-arrestin recruitment, increase ERK phosphorylation, and induce receptor internalization, and EC50 values for monkey, dog, rat, and mouse APJ were similar.
BMS-986224 induces a sustained increase in cardiac output in the cardiac disease setting and exhibits a differentiated profile from the renin-angiotensin system inhibitor enalapril.

物理化学性质&存储条件

分子量 498.92
分子式 C24H23ClN4O6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-(5-((5-chloropyridin-2-yl)methyl)-1,3,4-oxadiazol-2-yl)-5-(2,6-dimethoxyphenyl)-6-(ethoxymethyl)-4-hydroxypyridin-2(1H)-one

参考文献

1. Gargalovic P, et al. Circ Heart Fail. 2021 Mar;14(3):e007351.

2. Pi Z, et al. ACS Med Chem Lett. 2021 Oct 22;12(11):1766-1772.

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