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Chemical Structure| 142880-36-2 同义名 : GM6001;Galardin
CAS号 : 142880-36-2
货号 : A237914
分子式 : C20H28N4O4
纯度 : 99%+
分子量 : 388.461
MDL号 : MFCD00917040
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(115.84 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+40% PEG 300+2% Tween 80+water 11 mg/mL

生物活性
靶点

  • MMP

    MMP-2, Ki:0.1 nM

    MMP-26, Ki:0.36 nM
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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
临床研究
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 ... 展开 >> 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 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.87mL

2.57mL

1.29mL

25.74mL

5.15mL

2.57mL
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.