| 產(chǎn)品描述： | Ilomastat (GM6001) is a potent and broad spectrum matrix metalloprotease (MMP) inhibitor, inhibits MMPs (IC50s, 1.5 nM for MMP-1; 1.1 nM for MMP-2; 1.9 nM for MMP-3; 0.5 nM for MMP-9), with a Ki of 0.4 nM for human skin fibroblast collagenase (MMP-1). |
| 靶點(diǎn)： |
Fibroblast collagenase：0.4 nM (Ki, Human skin)；MMP-1：1.5 nM (IC50)；MMP-2：1.1 nM (IC50)；MMP-3：1.9 nM (IC50)；MMP-9：0.5 nM (IC50)；Thermolysin：20 nM (Ki)；Eastase：20 nM (Ki);MMP |
| 體內(nèi)研究： |
Ilomastat (GM6001) (400 μg/mL) inhibits corneal ulceration after severe alkali injury in animals. Ilomastat (GM6001) significantly suppresses intimal hyperplasia and intimalcollagen content. Ilomastat increases lumen area in stented arteries, shows no activity on proliferation rates in rabbit model after stenting |
| 參考文獻(xiàn)： |
1. Grobelny D, et al. Inhibition of human skin fibroblast collagenase, thermolysin, and Pseudomonas aeruginosa elastase by peptide hydroxamic acids. Biochemistry. 1992 Aug 11;31(31):7152-4. 2. Schultz GS, et al. Treatment of alkali-injured rabbit corneas with a synthetic inhibitor of matrix metalloproteinases. Invest Ophthalmol Vis Sci. 1992 Nov;33(12):3325-31. 3. Li C, et al. Arterial repair after stenting and the effects of GM6001, a matrix metalloproteinase inhibitor. J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8. 4. Leppert D, et al. T cell gelatinases mediate basement membrane transmigration in vitro. J Immunol. 1995 May 1;154(9):4379-89. 5. Yamamoto M, et al. Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket. J Med Chem. 1998 Apr 9;41(8):1209-17. |
| 溶解性： |
DMSO : ≥ 47 mg/mL (120.99 mM) |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.574 ml |
12.871 ml |
25.743 ml |
| 5 mM |
0.515 ml |
2.574 ml |
5.149 ml |
| 10 mM |
0.257 ml |
1.287 ml |
2.574 ml |
| 50 mM |
0.051 ml |
0.257 ml |
0.515 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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