AZD5462 | RXFP1 agonist | Probechem Biochemicals

Chemical Structure : AZD5462

CAS No.: 2787501-83-9

Catalog No.: 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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Biological Activity

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.

M.Wt	544.664
Formula	C30H41FN2O6
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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

1. Granberg KL, et al. J Med Chem. 2024 Mar 19. doi: 10.1021/acs.jmedchem.3c02184.