CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 ( G protein-coupled receptor kinase 2 ) inhibitor ( IC 50 =30 nM) while maintaining 230-fold selectivity over GRK5 ( IC 50 =7.09 μM) and more than 2500-fold selectivity over GRK1 ( IC 50 =
In Vitro:CCG258208 (Compound 14as) (0-1 μM; 10 min) shows significant improvement in βAR-stimulated contractility in mouse cardiomyocytes. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability Assay
In Vivo:CCG258208 (Compound 14as) (intraperitoneal injection; 10mg/kg; once) treatment shows superior half-life in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CD-1 mice Dosage: 10 m
Biological Activity:CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 ( G protein-coupled receptor kinase 2 ) inhibitor ( IC 50 =30 nM) while maintaining 230-fold selectivity over GRK5 ( IC 50 =7.09 μM) and more than 2500-fold selectivity over GRK1 ( IC 50 =