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首页-小分子抑制剂&激动剂-GPCR-Relaxin Receptor -AZD5462
AZD5462

Chemical Structure : AZD5462

CAS No.: 2787501-83-9

AZD5462 (AZD-5462)

货号: PC-49353Not For Human Use, Lab Use Only.

AZD5462 (AZD-5462) is a selective, allosteric, oral agonist of the Relaxin family peptide receptor 1 (RXFP1) with pEC50 of 7.8 (hRXFP1).

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

生物&药学活性

AZD5462 (AZD-5462) is a selective, allosteric, oral agonist of the Relaxin family peptide receptor 1 (RXFP1) with pEC50 of 7.8 (hRXFP1).
AZD5462 shows EC50 of 5.31 and 6.3 for Rat (rRXFP1cAMP) and mouse (muRXFP1cAMP) respectively.
AZD5462 displays >7 600-fold over class A human GPCRs (LGR4, LGR5, LGR6, LSHR (LHCGR), FSHR, TSHR and RXFP2) at Discovery X.
AZD5462 stimulates ERK phosphorylation in cells recombinantly expressing hRXFP1.
AZD5462 exhibits robust improvements in functional cardiac parameters in translatable cynomolgus monkey heart failure model.

物理化学性质&存储条件

分子量 544.664
分子式 C30H41FN2O6
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-4-methoxy-5-(((1S,2R,3S,4R)-3-(((1-methylcyclobutyl)methyl)carbamoyl)bicyclo[2.2.1]heptan-2-yl)carbamoyl)phenoxy)-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.3c02184.

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