产品
编 号:F624561
分子式:C27H23N5OS
分子量:465.57
产品类型
结构图
CAS No: 1337531-06-2
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产品详情
生物活性:
GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3.
体内研究:
GSK2593074A (GSK’074; 0.93?mg/kg/day; i.p. injection; 14 or 28 days) is administrated to Apoe-/- 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) .Animal Model:Apoe-/- female mice (9-10 months)
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.
体外研究:
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 IC50 of ~3?nM.