CCG258208
CAS No. : 2055990-90-2
(Synonyms: GRKs-IN-1)
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| Cat. No. : | HY-109562 |
| M.Wt: | 452.48 |
| Formula: | C24H25FN4O4 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research[1]. IC50 & Target: IC50: 30 nM (GRK2)[1]. In Vitro: CCG258208 (Compound 14as) (0-1 μM; 10 min) shows significant improvement in βAR-stimulated contractility in mouse cardiomyocytes[1]. In Vivo: CCG258208 (Compound 14as) (intraperitoneal injection; 10 mg/kg; once) treatment shows superior half-life in vivo[1].
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