PZ0236
CP-863187
≥98% (HPLC)
别名:
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
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About This Item
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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 10 mg/mL, clear
储存温度
room temp
SMILES字符串
FC1=C(C2=C(OC=N2)C(C=C3)=CN4C3=NN=C4C(C)C)C=C(F)C=C1
InChI
1S/C18H14F2N4O/c1-10(2)18-23-22-15-6-3-11(8-24(15)18)17-16(21-9-25-17)13-7-12(19)4-5-14(13)20/h3-10H,1-2H3
InChI key
UACOXBQBNWQWOK-UHFFFAOYSA-N
生化/生理作用
CP-863187 is a potent p38α (p38α) inhibitor (IC50 = 5.8 nM) with 44-fold selectivity over p38β (p38β) and no inhibitory potency against p38γ (p38γ) and p38δ (p38δ) isoforms. CP-863187 effectively inhibits LPS-stimulated cellular TNF-α 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).
CP-863187 is a potent p38α (p38α) inhibitor.
法律信息
Sold for research purposes under agreement from Pfizer Inc.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
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