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Medchemexpress LLC CCG258208 hydrochloride | 98.1% | 488.94 | 1 MG

Supplier: Medchemexpress LLC HY109562A10MM/1ML
CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM). It exhibits 230-fold selectivity over GRK5 and more than 2500-fold selectivity over GRK1, PKA, and ROCK1. This compound can be utilized in heart failure research.
- Potent and selective GRK2 inhibitor (IC50=30 nM).
- Exhibits 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1.
- Applicable in heart failure research.
- Significant improvement in βAR-stimulated contractility in mouse cardiomyocytes at concentrations as low as 0.1 μM.
- Superior half-life in vivo with total plasma drug levels exceeding the GRK2 IC50 for seven hours after a single intraperitoneal administration of 10 mg/kg in CD-1 mice.
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