AMG517

产品名称：

659730-32-2
AMG517
N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide
AMG 517
AMG-517
N-(4-(6-(4-(Trifluoromethyl)phenyl)pyrimidin-4-yloxy)benzo[d]thiazol-2-yl)acetamide

产品介绍：

产品说明

生化/生理作用

AMG517 is an orally active, highly potent and selective vanilloid receptor-1 (TRPV1; VR1; capsaicin receptor) antagonist that blocks TRPV1-mediated cellular Ca²⁺ influx (h/r/m IC₅₀/stimulant = 0.76 nM/1.01 nM/1.9 nM/500 nM capsaicin; 0.62 nM/0.5 nM/0.63 nM/acid (pH 5) using respective CHO transfectants; IC₅₀ >20 μM against TRPV2/3/4, TRPA1, and TRPM8-mediated responses; <45% binding at 10 μM to 87 receptors, enzymes, and ion channels) and exhibits antihyperalgesic efficacy in vivo (capsaicin-induced flinch = ED₅₀ = 0.33 mg/kg rats, p.o.; CFA-induced thermal hyperalgesia, MED = 0.83 mg/kg rats, p.o.).

基本信息

经验(实验)分子式	C₂₀H₁₃F₃N₄O₂S
分子量	430.40
MDL编号	MFCD14584859

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