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首页-小分子抑制剂&激动剂-GPCR-Relaxin Receptor -AZ7976
AZ7976

Chemical Structure : AZ7976

CAS No.: 2813866-27-0

AZ7976 (AZ-7976)

货号: PC-22033Not For Human Use, Lab Use Only.

AZ7976 (AZ-7976) is a potent, highly selective, allosteric relaxin family peptide receptor 1 (RXFP1) agonist with pEC50 of 9.4 in hRXFP1 cAMP assay in CHO-K1 cells, Emax=114%.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AZ7976 (AZ-7976) is a potent, highly selective, allosteric relaxin family peptide receptor 1 (RXFP1) agonist with pEC50 of 9.4 in hRXFP1 cAMP assay in CHO-K1 cells, Emax=114%.
AZ7976 binds to an allosteric site on RXFP1, does not compete with but rather enhance binding of 125I-relaxin H2.
AZ7976 is 500-fold less potent RXFP1 agonist in rat compared to human RXFP1.
AZ7976 increases heart rate achieving a Cmax at the rRXFP1cAMP EC50 elicited similar directional effects on these parameters as relaxin H2 in rodents.

物理化学性质&存储条件

分子量 682.65
分子式 C30H33F7N2O6S
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

(1S,4s)-4-(2-fluoro-5-(((1S,2R,3S,4R)-3-((4-fluoro-3-(pentafluoro-l6-sulfaneyl)phenyl)carbamoyl)bicyclo[2.2.1]heptan-2-yl)carbamoyl)-4-methoxyphenoxy)-1-methylcyclohexane-1-carboxylic acid

参考文献

1. Granberg KL, et al. J Med Chem. 2024 Mar 19. doi: 10.1021/acs.jmedchem.3c02183.

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