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CAS No. | 865608-11-3 | Cat. No. | BCP37871 |
Name | CMPD101 | ||
Synonyms | CMPD 101; CMPD-101; Takeda101; Takeda-101; Takeda 101; | ||
SMILES | CN1C(=NN=C1C2=CC=NC=C2)CNC3=CC=CC(=C3)C(=O)NCC4=CC=CC=C4C(F)(F)F | ||
Chemical Name | |||
Formula | C24H21F3N6O | M. Wt | 466.47 |
Purity | 98% | Storage | Store at 4-8°C |
Description | CMPD101 is a novel, potent and selective G-protein coupled receptor kinase 2 and 3 (GRK2/GRK3) inhibitor (IC50 values are 35 and 32 nM at GRK2 and GRK3 respectively). CMPD101 exhibits selectivity for GRK2/3 over GRK1/5 and reduces DAMGO-induced desensitization and internalization of μ-opioid receptors. CMPD101 has been shown to potentiate phosphatidylinositol 4,5-bisphosphate (PIP2) depletion and slow agonist-induced desensitization of protease-activated receptor 2 (PAR2). |
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