AZD5462 (Pexerelgon, AZD-5462)

Chemical Structure : AZD5462

CAS No.: 2787501-83-9

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

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

规格	价格	库存
5 mg	￥3280	In stock
10 mg	￥5280	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

AZD5462 (Pexerelgon, 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.