DATASHEET
Formulation
Powder
Storage:
Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 466.46
Formula: C24 H21 F3 N6 O
CAS Number: 865608-11-3
InChi Key: WFOVEDJTASPCIR-UHFFFAOYSA-N
InChi: InChI=1S/C24H21F3N6O/c1-33-21(31-32-22(33)16-9-11-28-12-10-16)15-29-19-7-4-6-17(13-19)23(34)30-14-18-5-2-3-8-20(18)24(25,26)27/h2-13,29H,14-15H2,1H3,(H,30,34)
Smiles: CN1C(=NN=C1CNC1C=C(C=CC=1)C(=O)NCC1C=CC=CC=1C(F)(F)F)C1C=CN=CC=1
Purity: 98.0
Solubility: Soluble in DMSO, not in water
Appearance: Solid Power.
Shelf Life: 1.0 years
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).