Ilomastat (Synonyms: 伊洛马司他; GM6001; Galardin)
目录号: PL07419 纯度: ≥98%
CAS No. :142880-36-2
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中文名称
Ilomastat
中文别名
伊洛马司他;Ilomastat (GM6001, Galardin) 抑制剂
英文名称
Ilomastat
英文别名
Butanediamide,N4-hydroxy-N1-[(1S)-1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl]-2-(2-methylpropyl)-,(2R)-;Butanediamide,N4-hydroxy-N1-[(1S)-1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl]-2-(2-met...;GM 6001 (Ilomastat,Galardin);Ilomastat;Ilomastat (GM6001, Galardin);(2R)-N~4~-hydroxy-N~1~-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide;(r)-n4-hydroxy-n1-[(s)-2-(1h-indol-3-yl)-1-methylcarbamoly-ethyl]-2-isobutyl-succinamide;(R)-N4-Hydroxy-N1-[(S)-2-(1H-indol-3-yl)-1-methylcarbamoyl-ethyl]-2-isobutyl-succinamide;Galardin;galardin tm;Galardin, GM6001, Ilomastat;GM-6001;GM6001;CS 610;(2R)-N4-Hydroxy-N1-[(1S)-1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl]-2-(2-methylpropyl)-butanediamide;GM 6001;Illomastat;I0403ML141;N-[(2R)-2-(Hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan Methylamide;(R)-N(sup 1)-Hydroxy-N-((S)-2-indol-3-yl-1-(methylcarbamoyl)ethyl)-2-isobutylsuccinamide;(S-(R*,S*))-N(sup 4)-Hydroxy-N(sup 1)-(1H-indol-3-ylmethyl)-2-(methylam
Cas No.
142880-36-2
分子式
C20H28N4O4
分子量
388.46
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Ilomastat (GM6001) 是一种有效、广谱的基质金属蛋白酶 (MMP) 抑制剂,能够抑制 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 值为 0.4 nM。
生物活性
Ilomastat (GM6001) is a potent and broad spectrum matrix metalloprotease (MMP) inhibitor, inhibits MMPs (IC 50 s, 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 K i of 0.4 nM for human skin fibroblast collagenase (MMP-1).
性状
Solid
IC50 & Target[1][2]
Fibroblast collagenase 0.4 nM (Ki, Human skin) MMP-1
体外研究(In Vitro)
Ilomastat (GM6001) inhibits human skin fibroblast collagenase, thermolysin and elastase with Kis of 0.4 nM, 20 nM, 20 nM, resepctively. Ilomastat (0.1-10 nM) inhibits gelatinase A and gelatinase B produced by T-cells. Ilomastat inhibits T-cell homing. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : ≥ 47 mg/mL (120.99 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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