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).
MedKoo Cat#: 523120
Name: CMPD101
CAS#: 865608-11-3
Chemical Formula: C24H21F3N6O
Exact Mass: 466.1729
Molecular Weight: 466.47
Elemental Analysis: C, 61.80; H, 4.54; F, 12.22; N, 18.02; O, 3.43
| Solvent | mg/mL | mM | comments | |
|---|---|---|---|---|
| Solubility | ||||
| DMF | 20.0 | 42.88 | ||
| Ethanol | 28.3 | 60.73 |
The following data is based on the product molecular weight 466.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
