SKF96365 (TRPC抑制剂)

化学名

1-[2-(4-methoxyphenyl)-2-[3-(4-methoxyphenyl)propoxy]ethyl]imidazole;hydrochloride

简称

SKF96365

别名

SK and F 96365, SK and F-96365, SKF-96365, SKF 96365, SKF 96365 HYDROCHLORIDE

中文名

N/A

化学式

C₂₂H₂₆N₂O₃.HCl

分子量

402.91

CAS号

130495-35-1

纯度

98%

溶剂/溶解度

Water80mg/ml; DMSO80mg/ml; Ethanol80mg/ml

溶液配制

5mg加入1.24ml DMSO，或者每4.03mg加入1ml DMSO，配制成10mM溶液。SF1159-10mM用DMSO配制。

产品描述

SKF96365, originally identified as a blocker of receptor-mediated calcium entry, is widely used diagnostically, as a blocker of transient receptor potential canonical type (TRPC) channels.

信号通路

Others

靶点

TRPC

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－

－

－

IC50

－

－

－

－

－

体外研究

SKF-96365 exhibits protective activity against MPP+ injury in PC12 cells and significantly inhibits apoptotic cell death in PC12 cells after MPP+ administration. SKF-96365 does not exert effects on necrotic cell death induced by MPP+ insult in PC12 cells. Because of its non-selective activity, SKF-96365 has been demonstrated to have effects on multiple other Ca²⁺ channels: it not only blocks high-voltage-activated (HVA) Ca²⁺ channels at typically utilized test concentrations, but also potently inhibits low-voltage -activated (LVA) T-type Ca²⁺ channels in HEK293 cells. The exact effect of SKF-96365 on intracellular calcium homeostasis might dependent on cell types and experimental models used.

体内研究

SKF-96365 treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo.

临床实验

N/A

特征

N/A

酶活性检测实验

方法

N/A

细胞实验

细胞系

PC12 cells

浓度

1μM, 10μM, 50μM

处理时间

30 min

方法

To investigate whether SKF-96365 could protect PC12 cells from injury induced by MPP+ insult, cultured PC12 cells are pretreated with SKF-96365 in different concentrations (1μM, 10μM or 50μM) 30 min before MPP+ addition. The cells viability is measured 24h after MPP+ insult by using the cell proliferation reagent WST-1.

动物实验

动物模型

C57BL/6N mice

配制

0.9% sterile saline

剂量

0.02μMol-0.2μMol/2μl/mouse

给药方式

intrastriatally

产品编号

产品名称

包装

SF1159-10mM

SKF96365 (TRPC抑制剂)

10mM×0.2ml

SF1159-5mg

SKF96365 (TRPC抑制剂)

5mg

SF1159-25mg

SKF96365 (TRPC抑制剂)

25mg

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说明书

1份