GM6001

GM6001CAS号: 142880-36-2分子式: C20H28N4O4分子量: 388.46描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

GM6001 (galardin, ilomastat)是泛MMP抑制剂,对MMP-1,MMP-2,MMP-3,MMP-7,MMP-8,MMP-9,MMP-12,MMP-14和MMP-26的Ki为0.4-27 nM。

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
伊洛马司他;Ilomastat;Galardin
外观
off-white powder
可溶性/溶解性
DMSO : 38.9 mg/mL (100 mM)
生物活性
靶点
MMP-8 ,MMP-9 ,MMP-26 ,MMP-1 ,MMP-2
In vitro(体外研究)
GM6001 inhibits human skin fibroblast collagenase with Ki of 0.4 nM when assayed with a synthetic thio ester substrate at pH 6.5, with 50-fold selectivity over two bacterial enzymes, thermolysin and Pseudomonas aeruginosa elastase. GM 6001 (0.1 nM – 10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, thus inhibits T-cell homing.
In vivo(体内研究)
Topical application of GM6001 (400 μg/ml) prevents corneal ulceration after severe alkali injury. In rabbit model after stenting, GM6001 significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates.

分子结构图

GM6001