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CAS No.: 142880-36-2

Ilomastat/伊洛马司他 Catalog No. CSN11187

Synonyms: GM6001;Galardin;伊洛马司他

GM6001 is a broad spectrum MMPs inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM, respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 MMP1

Ki:0.4nM MMP12

Ki:3.6nM MMP14

Ki:13.4nM MMP2

Ki:0.5nM MMP26

Ki:0.36nM 更多
描述GM 6001 is a broad spectrum MMP inhibitor with Ki values of 0.1nM, 0.2nM, 0.36nM, 0.4nM, 0.5nM, 3.6nM and 3.7nM for MMP-8, MMP-9, MMP-26, MMP-1, MMP-2, MMP-12 and MMP-7^[1]. The tyrosine phosphorylation of EGFR induced by leptin could be significantly attenuated by treatment with 25μM GM6001 for 30min in rat aortic smooth muscle cells, due to the inhibition of proteolytic cleavage of transmembrane precursors via matrix metalloproteinase by GM6001^[2]. Inhibition of MMP-2/MMP-9-mediated NCAM (Neural cell adhesion molecule) proteolysis by administration of 5μg GM6001 through intracerebroventricular route 30 minutes before and 2 h after ischemia attenuated the infarction, behavioral abnormalities of MCAO (middle cerebral artery occlusion) model mice, with suppression on the level of NCAM cleavage product by GM6001 observed^[3].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HEk293 cells	-	Function assay	-	Inhibition of human recombinant ADAMTS4 expressed in HEk293 cells using FAM-AEwLQGRPISIAK-TAMRA as substrate measured for 15 mins by fluorometric analysis, IC50=0.48 μM	23376997
human U251 cells	20 μM	Function assay	-	Protection against anthrax PA63-lethal toxin complex-induced cytotoxicity in human U251 cells at 20 uM at 400 ng/ml by MTT test	17537721

动物研究
剂量
Hamster: 20 mg/kg^[4] (i.p.) Rat: 1.2 mg/kg^[5] (i.p.); 50 mg/kg, 100 mg/kg^[6] (i.p.)

给药途径
i.p.
临床研究

动物研究
剂量	Hamster: 20 mg/kg^[4] (i.p.) Rat: 1.2 mg/kg^[5] (i.p.); 50 mg/kg, 100 mg/kg^[6] (i.p.)
给药途径	i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03297827	-	-	Recruiting	August 27, 2019	United States, New Mexico ... more >> Department of Neurology, University of New Mexico Recruiting Albuquerque, New Mexico, United States, 87131-0007 Contact: Asad Ikram, MD 505-272-9382 aikram@salud.unm.edu Principal Investigator: Atif Zafar, MD Sub-Investigator: Asad Ikram, MD Collapse <<

参考文献

[1] Grobelny D, Poncz L, 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] Chao HH, Hong HJ, et al. Leptin stimulates endothelin-1 expression via extracellular signal-regulated kinase by epidermal growth factor receptor transactivation in rat aortic smooth muscle cells. Eur J Pharmacol. 2007 Nov 14;573(1-3):49-54. Epub 2007 Jul 4.
[3] Shichi K, Fujita-Hamabe W, et al. Involvement of matrix metalloproteinase-mediated proteolysis of neural cell adhesion molecule in the development of cerebral ischemic neuronal damage. J Pharmacol Exp Ther. 2011 Aug;338(2):701-10.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5743 mL
- 12.8713 mL
- 25.7426 mL
- 5 mM
- 0.5149 mL
- 2.5743 mL
- 5.1485 mL
- 10 mM
- 0.2574 mL
- 1.2871 mL
- 2.5743 mL

技术信息

CAS号

142880-36-2

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H28N4O4

运输

蓝冰

分子量

388.46

别名

GM6001;Galardin;伊洛马司他

溶解度

DMSO	50.0 mg/mL (128.7 mM)
Water	insoluble

动物实验配方

2% DMSO+40% PEG 300+2% Tween 80+water

11 mg/mL

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靶点	Description	IC50
MMP1		Ki:0.4nM
MMP12		Ki:3.6nM
MMP14		Ki:13.4nM
MMP2		Ki:0.5nM
MMP26		Ki:0.36nM
MMP3		Ki:27nM
MMP7		Ki:3.7nM
MMP8		Ki:0.1nM
MMP9		Ki:0.2nM

Ilomastat/伊洛马司他 Catalog No. CSN11187

靶点选择性

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