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Medchemexpress LLC CCG258208 hydrochloride | 98.1% | 488.94 | 25 MG
Supplier: Medchemexpress LLC 25MGHY109562A
CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective inhibitor of GRK2 (G protein-coupled receptor kinase 2) with an IC50 of 30 nM. It demonstrates significant selectivity, being 230-fold more selective over GRK5 (IC50=7.09 μM) and over 2500-fold more selective over GRK1 (IC50=87.3 μM), PKA, and ROCK1. This compound is utilized in heart failure research.
- Potent and selective GRK2 inhibitor (IC50=30 nM).
- High selectivity over GRK5 (230-fold).
- Even higher selectivity over GRK1, PKA, and ROCK1 (more than 2500-fold).
- Applicable in heart failure research.
- Shows significant improvement in βAR-stimulated contractility in mouse cardiomyocytes at concentrations as low as 0.1 μM.
- Exhibits a superior half-life *in vivo*.
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