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AZD5462

Names

[ CAS No. ]:
2787501-83-9

[ Name ]:
AZD5462

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Others >> Others

[Target]

RXFP1[1]


[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C30H41FN2O6

[ Molecular Weight ]:
544.65

Related Compounds