GSK-7975A - CAS:1253186-56-9 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	GSK-7975A
英文名称:	GSK-7975A
别名:	GSK-7975A GSK-7975A
CAS No:	1253186-56-9	分子式:	C₁₈H₁₂F₅N₃O₂	分子量:	397.3
CAS No:	1253186-56-9
分子式:	C₁₈H₁₂F₅N₃O₂
分子量:	397.3

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G10561 GSK-7975A ≥98% (psaitong)

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包装规格：

5mg 10mg 25mg 50mg 100mg in glass bottle

溶解性：

溶于DMSO(≥90mg/ml)

产品描述：

基本信息

产品编号：	G10561
产品名称：	GSK-7975A
CAS:	1253186-56-9	储存条件	粉末	-20℃	四年

分子式：	C18H12F5N3O2		溶于液体	-80℃	6个月
分子量：	397.30			-20℃	1个月
化学名：	2,6-difluoro-N-[1-[[4-hydroxy-2-(trifluoromethyl)phenyl]methyl]pyrazol-3-yl]benzamide
Solubility (25°C)：
体外:	DMSO
	Ethanol
	Water
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.5170mL	12.5849mL	25.1699mL
5mM	0.5034mL	2.5170mL	5.0340mL
10mM	0.2517mL	1.2585mL	2.5170mL

生物活性

产品描述	一种高效有口服活性的CRAC通道抑制剂。
靶点	Calcium Channel
体外研究	GSK-7975A reduces FcεRI-dependent Ca2+ influx and 3μM GSK-7975A reduces the release of histamine,leukotriene C4,and cytokines (IL-5/-8/-13 and TNFα) by up to 50%.GSK-7975A inhibits mediator release from mast cells,and proinflammatory cytokine release from T-cells in a variety species.GSK-7975A completely inhibits calcium influx through CRAC channels.This leads to inhibition of the release of mast cell mediators and T-cell cytokines from multiple human and rat preparations.Mast cells from guinea-pig and mouse preparations are not inhibited by GSK-7975A;however cytokine release is fully blocked from T-cells in a mouse preparation.GSK-7975A inhibits toxin-induced activation of ORAI1 and/or activation of Ca2+ currents after Ca2+ release,in a concentration-dependent manner,in mouse and human pancreatic acinar cells (inhibition >90% of the levels observed in control cells).GSK-7975A also prevents activation of the necrotic cell death pathway in mouse and human pancreatic acinar cells.
体内研究	GSK-7975A inhibits local and systemic features of acute pancreatitis in TLCS-AP,CER-AP,FAEE-AP,in dose- and timedependent manners.GSK-7975A significantly reduces increases in serum amylase,IL6,and pancreatic MPO levels;lung MPO is reduced significantly by low dose only.GSK-7975A markedly reduces pancreatic histopathology in TLCS-AP,CER-AP,and FAEE-AP.

推荐实验方法(仅供参考)

动物实验:

Mice:Acute pancreatitis is induced in C57BL/6J mice by ductal injection of taurolithocholic acid 3-sulfate or intravenous'administration of cerulein or ethanol and palmitoleic acid.Some mice then are given GSK-7975A,which inhibit ORAI1,at different time points to assess local and systemic effects.Sampling of GSK-7975A is at 1,2,4,10,and 22 hours after osmotic minipump insertion from 3 mice/time point.Immediately after humane killing,blood is collected into a heparinized tube,diluted 1:1 with sterile water,and the pancreas is removed and homogenized.Standards and study samples (50μL from blood and 100μL from pancreas) are extracted by protein precipitation and centrifuged.Supernatants are dried under heated nitrogen (40℃).Levels of GSK-7975A and GSK-6288B are determined.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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