Synonyms: 4-(2,5-Difluorophenyl)-5-(3-isopropyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxazole; 6-[4-(2,5-Difluorophenyl)-5-oxazolyl]-3-(1-methylethyl)-1,2,4-triazolo[4,3-a]pyridine; 6-[4-(2,5-Difluorophenyl)oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; CP863187
Molecular Formula: C18H14F2N4O
Molecular Weight: 340.33
Linear Structural Formula: C18H14F2N4O
MDL Number: MFCD30480740
Purity: >=98% (HPLC)
Storage: room temp
Biochem Physiol Actions: CP-863187 is a potent p38alpha (p38alpha) inhibitor (IC50 = 5.8 nM) with 44-fold selectivity over p38beta (p38beta) and no inhibitory potency against p38gamma (p38gamma) and p38delta (p38delta) isoforms. CP-863187 effectively inhibits LPS-stimulated cellular TNF-alpha production in vitro (IC50 = 259 and 25 nM, using human whole blood and isolated mononuclear cells, respectively) and in rats in vivo (ED50 = 0.3 mg/kg p.o.) with good pharmacokinetic profile and oral availability (F = 87%/dog, 40%/monkey, 30%/rat with 5 mg/kg oral dosage; F = 66%/rat with 50 mg/kg oral dosage).
Legal Information: Sold for research purposes under agreement from Pfizer Inc.