产品说明
生化/生理作用
AM-0902 (AMG0902) is a potent and selective transient receptor potential A1 (TRPA1) antagonist (rat/human TRPA1 IC50 = 71/131 nM against AITC-induced 45Ca2+ influx in respective CHO transfectants with [AITC] = EC90 = 3 μM/hTRPA1 or 35 μM/rTRPA1; human/rat IC50 = 24/20 nM by FLIPR) with little potency against human TRPV1/4, human CYP3A4/2D6, rat TRPV1/3, rat TRPM8, or mouse NaV1.7. AM-0902 effectively reduces AITC-induced flinching in a rat pain model (by 65% and 85%, respectively, with 10 or 30 mg/kg AM-0902 p.o. 1 hr prior to AITC injection) with good pharmacokinetic properties, oral availability and brain exposure (F = 60%, B/P = 0.2; 30 mg/kg p.o. in rats) in vivo.
基本信息
经验(实验)分子式 | C17H15ClN6O2 |
分子量 | 370.79 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
颜色 | white to beige |
溶解性 | DMSO: 2 mg/mL, clear |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |