Synonyms: 3-(1,1-Dimethylethyl)-6-[4-(2,4,5-trifluorophenyl)-5-oxazolyl]-1,2,4-triazolo[4,3-a]pyridine; 3-tert-Butyl-6-[4-(2,4,5-trifluorophenyl)-1,3-oxazol-5-yl][1,2,4]triazolo[4,3-a]pyridine; 3-tert-Butyl-6-[4-(2,4,5-trifluorophenyl)oxazol-5-yl]-[1,2,4]triazolo[4,3-a]pyridine; 5-(3-tert-Butyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-4-(2,4,5-trifluorophenyl)oxazole; CP944629
Molecular Formula: C19H15F3N4O
Molecular Weight: 372.34
Linear Structural Formula: C19H15F3N4O
Purity: >=98% (HPLC)
Storage: room temp
Biochem Physiol Actions: CP-9446219 is a potent p38alpha (p38alpha) inhibitor (IC50 = 1.8 nM) with no inhibitory potency against a panel of 26 other knases (IC50 >10 muM), including p38gamma (p38gamma) and p38delta (p38delta), MKK1, MAPK2/ERK2, JNK, MAPKAP-K1a, and MAPKAP-K2. CP-944629 effectively inhibits LPS-stimulated cellular TNF-alpha production in vitro (IC50 = 63 and 8.3 nM, using human whole blood and isolated mononuclear cells, respectively) and in rats in vivo (ED50 = 0.1 mg/kg p.o.) with good pharmacokinetic profile and oral availability (F = 66%/monkey, 54%/rat).
Legal Information: Sold for research purposes under agreement from Pfizer Inc.