GSK2593074A - CAS:1337531-06-2

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GSK2593074A (Synonyms:GSK'074)

目录号 : KM2910 CAS No. : 1337531-06-2

Data Sheet 产品使用指南

GSK2593074A (GSK’074) 是一种程序性坏死 (necroptosis) 抑制剂, 抑制 RIP1 和 RIP3。

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500mg	询价	In-stock

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生物活性

GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3.

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.

Cell Viability Assay

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 IC₅₀ of 3 nM.

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.

分子式

C₂₇H₂₃N₅Os

分子量

465.57

CAS号

1337531-06-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg	5 mg	10 mg

1 mM	2.1479 mL	10.7395 mL	21.4790 mL
5 mM	0.4296 mL	2.1479 mL	4.2958 mL
10 mM	0.2148 mL	1.0740 mL	2.1479 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。