CCG258208 hydrochloride (compound 14as hydrochloride) is a highly potent and selective G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 30 nM. It exhibits >200-fold selectivity for GRK2 over GRK5 (IC50 = 7.1µM). In cardiovascular research, CCG258208 effectively enhances the contractility of beta-AR-stimulated cardiomyocytes by inhibiting GRK2 activity. Additionally, the compound demonstrates excellent in vivo stability, making it a valuable tool for studying GRK2-related conditions such as heart failure.
Molecular Weight:
488.94
Formula:
C24H26ClFN4O4
Target:
GRK
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