Ilomastat 是广谱的基质金属蛋白酶 (MMP) 抑制剂，可抑制 MMP 的活性，IC50值分别为 1.5 nM (MMP-1)，1.1 nM (MMP-2)，1.9 nM (MMP-3)，0.5 nM (MMP-9)，对人皮肤成纤维细胞胶原酶 (MMP-1) 的Ki=为 0.4 nM。

Ilomastat (GM6001, Galardin) is a broad spectrum matrix metalloprotease (MMP) inhibitor.

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. [4]

Collagenase assay uses the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5. The collagenase concentration is 1-2 nM, and the substrate concentrations are from 0.1 to 0.7 nM. Km?is found to vary between 1.5 and 4 mM.

142880-36-2

C20H28N4O4

388.468

GM6001;Galardin;伊洛马司他

DMSO:38.9 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years