Ilomastat-GM6001-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIlomastatCat. No.: HY-15768CAS No.: 142880-36-2Synonyms: GM6001; Galardin分式: CHNO分量: 388.46作靶点: MMP作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 47 mg/mL (12

2、0.99 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5743 mL 12.8713 mL 25.7427 mL5 mM 0.5149 mL 2.5743 mL 5.1485 mL10 mM 0.2574 mL 1.2871 mL 2.5743 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Ilomastat (GM6001)种有效、谱的 质属蛋酶 (MMP

3、) 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)，对肤成纤维细胞胶原酶 (MMP-1) 的 Ki 值为 0.4 nM。IC50 & Target MMP-9 MMP-2 MMP-1 MMP-31/3 Master of Small Molecules 您边的抑制剂师www.MedChemE0.5 nM (IC50) 1.1 nM (IC50) 1.5 nM (IC50) 1.9 nM (IC50)Fibroblast collagenase Thermolysin

4、Eastase0.4 nM (Ki, Human skin) 20 nM (Ki) 20 nM (Ki)体外研究 Ilomastat (GM6001) inhibits human skin fibroblast collagenase, thermolysin and elastase with Kis of 0.4 nM,20 nM, 20 nM, resepctively 1. Ilomastat (0.1-10 nM) inhibits gelatinase A and gelatinase B produced by T-cells. Ilomastat inhibits T-cel

5、l homing 4.体内研究 Ilomastat (GM6001) (400 g/mL) inhibits corneal ulceration after severe alkali injury in animals 2. Ilomastat(GM6001) significantly suppresses intimal hyperplasia and intimalcollagen content. Ilomastat increaseslumen area in stented arteries, shows no activity on proliferation rates i

6、n rabbit model after stenting 3.PROTOCOLAnimal To assess the effects of MMP inhibition, animals are given daily injections of either vehicle (“placebo group”)Administration 3 or Ilomastat (GM6001) (100 mg/kg per day as subcutaneous suspension), beginning one day before thesecond injury until seven d

7、ays after the procedure. Ilomastat (GM6001) is a nonspecific hydroxamic acid-based MMPI with potent inhibitory activity against collagenase, gelatinases and stromelysin. Animals areeuthanized at either 1 week or 10 weeks after the second injury. For biochemical studies, iliac artery tissue isremoved

8、 under general anesthetic, followed by a fatal intracardiac injection of thiopentol. Forhistomorphometric studies, iliac arteries are perfusion-fixed in 10% buffered formalin for 20 min at a perfusionpressure of 80 mm Hg.MCE has not independently confirmed the accuracy of these methods. They are for

9、 reference only.户使本产品发表的科研献 Nat Commun. 2017 Mar 7;8:14483. Biomaterials. 2018 Aug 22;183:67-76. Proc Natl Acad Sci U S A. 2016 Sep 27;113(39):11004-9. Int J Nanomedicine. 2018 Aug 13;13:4641-4659. Int J Nanomedicine. 2016 Apr 22;11:1643-61.See more customer validations on HYPERLINK / www.MedChemERE

10、FERENCES1. Grobelny D, et al. Inhibition of human skin fibroblast collagenase, thermolysin, and Pseudomonas aeruginosa elastase by peptidehydroxamic 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 me

11、talloproteinases. Invest Ophthalmol VisSci. 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 Jun5;39(11):1852-8.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE4. Leppert D, et al. T cell

12、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 subsitepocket. J Med Chem. 1998 Apr 9;41(8):1209-17.McePdfHeightCaution: Pr