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GSK2593074A
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK2593074A图片
CAS NO:1337531-06-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
GSK2593074A (GSK'074) 是一种程序性坏死 (necroptosis) 抑制剂, 抑制 RIP1 和 RIP3。
Cas No.1337531-06-2
别名GSK'074
分子式C27H23N5OS
分子量465.57
溶解度DMSO : 41.67 mg/mL (89.50 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GSK2593074A (GSK'074) is anecroptosisinhibitor with dual targeting ability to bothRIP1andRIP3[1].

GSK2593074A (GSK'074; 0.01, 0.1, 1, 10, and 100 nM; 6 hours for MOVAS cells; 3 hours for L929 cells) completely rescues cells from necroptosis under different stimuli in both human and murine cells at IC50~3 nM. In multiple cell types including mouse SMCs, fibroblasts (L929), bone marrow derived macrophages (BMDM), and human colon epithelial cells (HT29), GSK2593074A inhibits necroptosis with an IC50of ~3 nM[1].

Cell Viability Assay[1]

Cell Line:Mouse smooth muscle cell line MOVAS; Mouse fibroblast cell line L929
Concentration:0.01, 0.1, 1, 10, and 100 nM
Incubation Time:6 hours for MOVAS cells; 3 hours for L929 cells
Result:Inhibited MOVAS and L929 cells with the IC50of 3 nM.

GSK2593074A (GSK'074; 0.93 mg/kg/day; i.p. injection; 14 or 28 days) is administrated toApoe-/-mice immediately following pump implantation. Compared to the DMSO group, GSK2593074A-treated mice show significantly alleviated aneurysm formation, reflected by a much smaller aortic dilatation (DMSO 85.39±15.76% vs GSK2593074A 36.28±5.76%; P<0.05) as well as a reduced abdominal aortic aneurysm (AAA) incidence (from 83.3 to 16.7%). GSK2593074A significantly decreases the extent of aortic expansion (DMSO 66.06±9.17% vs GSK2593074A 27.36±8.25%; P<0.05)[1].

Animal Model:Apoe-/-female mice (9-10 months)[1]
Dosage:0.93 mg/kg/day; 200 µL
Administration:Daily i.p. injection; 14 or 28 days
Result:Inhibited aneurysm formation in mouse models of aneurysms.