Ilomastat,GM6001,Galardin142880-36-2 伊洛马司他(GM6001)

伊洛马司他(GM6001)

分子式：C20H28N4O4   分子量：388.46

 

产品描述

GM6001 (galardin, ilomastat) 是广谱matrix metalloprotease (MMP)YZ剂，作用于MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, 和 MMP-26，Ki分别为0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 和0.36 nM。

靶点

MMP

         

IC50

0.4-27 nM (Ki)

         

体外研究

GM 600l 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.

体内研究

Topical application of GM6001 (400 μg/ml) prevents corneal ulceration after severe alkali injury. [3] 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.

溶解性

DMSO ≥25 mM，乙醇 10 mg/ml

稳定性

2年 -20°C粉状，6月-80°C溶于DMSO