Bioactivity | 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]. |
Target | RXFP1 |
Invitro | 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]. |
Name | AZD5462 |
CAS | 2787501-83-9 |
Formula | C30H41FN2O6 |
Molar Mass | 544.65 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
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. |