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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)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
GSK'074
产品介绍
GSK2593074A (GSK’074) 是一种程序性坏死 (necroptosis) 抑制剂, 抑制RIP1RIP3
生物活性

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

IC50& Target

RIP1, RIP3[1]

体外研究
(In Vitro)

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.
体内研究
(In Vivo)

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.
分子量

465.57

性状

Solid

Formula

C27H23N5OS

CAS 号

1337531-06-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 41.67 mg/mL(89.50 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1479 mL10.7395 mL21.4790 mL
5 mM0.4296 mL2.1479 mL4.2958 mL
10 mM0.2148 mL1.0740 mL2.1479 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.47 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。