Synonyms: 3-((4-Methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methylamino)-N-(2-(trifluoromethyl)benzyl)benzamide; 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide hydrochloride; Compound 101 hydrochloride; Cpd101 hydrochloride; Takeda101 hydrochloride
Molecular Formula: C24H21N6OF3 · HCl
Molecular Weight: 502.92
Linear Structural Formula: C24H21N6OF3 · HCl
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: CMPD101 is an active site-targeting, potent and subtype-selective G protein-coupled receptor kinase GRK2 & GRK3 inhibitor (human GRK2/3 IC50 = 54/32 nM with 3 muM ATP and tubulin dimer as substrate; bovine GRK2 IC50 = 290 nM with 0.5 mM ATP and bROS as substrate; no GRK1/5 inhibition at 125 muM). CMPD101 selectively inhibits GPR39 agonist-induced beta-arrestin recruitment (by 94% at 10 muM against 30 muM GPR39-C3/50 muM ZnCl2), but not cAMP pathway desensitization in cultures and prevents beta-arrestin2-biased D2R ligand UNC9994(1 mug/side bilateral local injection) from blocking NMDAR antagonist PCP (6 mg/kg i.p.)-induced locomotion (60%/12% blockage without/with 0.5 mug CMPD101 co-injection) in mice in vivo.