AMG986 (Azelaprag, AMG-986)

Chemical Structure : AMG986

CAS No.: 2049980-18-7

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货号: PC-38136Not For Human Use, Lab Use Only.

AMG986 (Azelaprag, AMG-986) is a small-molecule agonist of Apelin receptor (APJ, APLNR), inhibits forskolin-stimulated cAMP production (pEC50=9.64) and promoted Gα protein activation (pEC50=9.54).

规格	价格	库存
5 mg	￥1580	In stock
10 mg	￥2480	In stock
25 mg	￥4280	In stock
50 mg	￥7280	In stock
100 mg		Get quote

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生物&药学活性

AMG986 (Azelaprag, AMG-986) is a small-molecule agonist of Apelin receptor (APJ, APLNR), inhibits forskolin-stimulated cAMP production (pEC50=9.64) and promoted Gα protein activation (pEC50=9.54).
AMG986 is a full APJ agonist that exhibits slight differences in potency relative to one another and may be more potent when compared with the endogenous ligand pyr-apelin-13.
AMG986 exhibited a potentcy to recruit β-arrestin using the PathHunter arrestin assay with pC50 of 9.61.
AMG986 altered cardiac hemodynamics and increased cardiac reserve during dobutamine challenge in a rat model of impaired metabolic function and exhibited improved pharmacokinetic profile relative to pyr-apelin-13.

物理化学性质&存储条件

分子量	523.612
分子式	C25H29N7O4S
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	(2S,3R)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methyl-3-pyridinyl)-4H-1,2,4-triazol-3-yl)-3-(5-methyl-2-pyrimidinyl)-2-butanesulfonamide

参考文献

1. Brandon Ason, et al. JCI Insight. 2020 Apr 23;5(8):e132898.