产品
编 号：F252614
分子式：C24H25FN4O4
分子量：452.48
分子式：C24H25FN4O4
分子量：452.48
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CAS No: 2055990-90-2
产品详情
生物活性：
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.
体内研究：
CCG258208 (Compound 14as) (intraperitoneal injection; 10 mg/kg; once) treatment shows superior half-life in vivo.Animal Model:CD-1 mice
Dosage:10 mg/kg
Administration:Intraperitoneal injection; 10 mg/kg; once
Result:Showed total plasma drug levels after single IP administration that exceed the GRK2 IC50 for seven hours.
体外研究：
CCG258208 (Compound 14as) (0-1 μM; 10 min) shows significant improvement in βAR-stimulated contractility in mouse cardiomyocytes.
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.
体内研究：
CCG258208 (Compound 14as) (intraperitoneal injection; 10 mg/kg; once) treatment shows superior half-life in vivo.Animal Model:CD-1 mice
Dosage:10 mg/kg
Administration:Intraperitoneal injection; 10 mg/kg; once
Result:Showed total plasma drug levels after single IP administration that exceed the GRK2 IC50 for seven hours.
体外研究：
CCG258208 (Compound 14as) (0-1 μM; 10 min) shows significant improvement in βAR-stimulated contractility in mouse cardiomyocytes.
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