For research use only. Not for therapeutic Use.
AZD5462 is a RXFP1 modulator, can be used for heart failure research. RXFP1 is the cognate receptor for human relaxin, belongs to GPCR family 1c number with anti-fibrotic and anti-inflammatory properties[1].
AZD5462 (example 1) shows stimulatory activity on cAMP or cGMP production with EC50s of 17 nM and 50 nM, respectively[1].
AZD5462 binds human plasma protein with fraction unbound (free) rate of 4.3%, and shows the stability with Clint values of 23 μL/min/mg (human licer microsomal), 4.8 μL/min/106 cells (human hepatocyte), and 11 μL/min/106 cells (rat hepatocyte)[1].
AZD5462 enhances phosphorylation of ERK with an EC50 value of 6.3 nM[1].
| Catalog Number | I042894 |
| CAS Number | 2787501-83-9 |
| Synonyms | 4-[2-fluoro-4-methoxy-5-[[(1S,2R,3S,4R)-3-[(1-methylcyclobutyl)methylcarbamoyl]-2-bicyclo[2.2.1]heptanyl]carbamoyl]phenoxy]-1-methylcyclohexane-1-carboxylic acid |
| Molecular Formula | C30H41FN2O6 |
| Purity | ≥95% |
| InChI | InChI=1S/C30H41FN2O6/c1-29(9-4-10-29)16-32-27(35)24-17-5-6-18(13-17)25(24)33-26(34)20-14-23(21(31)15-22(20)38-3)39-19-7-11-30(2,12-8-19)28(36)37/h14-15,17-19,24-25H,4-13,16H2,1-3H3,(H,32,35)(H,33,34)(H,36,37)/t17-,18+,19?,24+,25-,30?/m1/s1 |
| InChIKey | LYUYYIGCZIZIGF-SRHODNEWSA-N |
| SMILES | CC1(CCC1)CNC(=O)C2C3CCC(C3)C2NC(=O)C4=CC(=C(C=C4OC)F)OC5CCC(CC5)(C)C(=O)O |
| Reference | [1]. Granberg Kenneth Lars, et al. 4-(2-Fluoro-4-methoxy-5-(3-(((1-methylcyclobutyl)methyl)carbamoyl)bicyclo[2.2.1]heptan-2-yl)carbamoyl)phenoxy)-1-methylcyclohexane-1-carboxylic acid derivatives and similar compounds as RXFP1 modulators for the treatment of heart failure and their preparation: World Intellectual Property Organization, WO2022122773. 2022-06-16. |
