|1-(2-(4-甲氧基苯基)-2-(3-(4-甲氧基苯基)丙氧基)乙基)-1H-咪唑盐酸盐|CsnPharm

CAS No.: 130495-35-1

1-(2-(4-Methoxyphenyl)-2-(3-(4-methoxyphenyl)propoxy)ethyl)-1H-imidazole hydrochloride Catalog No. CSN11934

Synonyms: SKF 96365 (hydrochloride);SKF-96365;SKF-96,365

SKF-96365 HCl is a transient receptor potential canonical type (TRPC) channel blocker, also bolcks voltage-gated Ca2+ channels and potassium channels.

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技术信息

生物活性

描述SKF-96365 Hydrochloride is the hydrochloride form of SKF-96365. SKF-96365 is a TRPC channel blocker, a potent LVA T-type Ca channels blocker and a SOCE (Store-operated Ca²⁺ entry) inhibitor, with IC50 values of 8.5μM and 11.7μM for inhibition of RMCE by SKF-96365 in platelets stimulated with ADP and thrombin, and IC50 value of ~560nM for human Ca_V3.1 T-type Ca channels. It can inhibit STIM1 and voltage-gated Ca²⁺ channels as well as potassium channels. SKF-96365 could be used as a tool to distinguish RMCE from internal Ca²⁺ release, and to probe the role of RMCE in mediating functional responses of cells. It inhibited native Ca_V3.1 T-type currents in a rat cerebellar PC slice preparation at 1 and 10μM. SKF-96365 inhibited STIM1-mediated Ca²⁺ influx and the nuclear translocation and activation of the NFAT transcription factor in cells expressing a constitutively active (EF-hand mutant) STIM1, suggesting it targets the STIM1-Orai1 pathway.
动物研究
剂量
Mice: 20 mg/kg^[4] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 20 mg/kg^[4] (i.p.)
给药途径	i.p.

[1] Várnai P, Hunyady L, et al. STIM and Orai: the long-awaited constituents of store-operated calcium entry. Trends Pharmacol Sci. 2009 Mar;30(3):118-28.
[2] Singh A, Hildebrand ME, et al. The transient receptor potential channel antagonist SKF96365 is a potent blocker of low-voltage-activated T-type calcium channels. Br J Pharmacol. 2010 Jul;160(6):1464-75.
[3] Merritt JE, Armstrong WP, et al. SK&F 96365, a novel inhibitor of receptor-mediated calcium entry. Biochem J. 1990 Oct 15;271(2):515-22.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4819 mL
- 12.4096 mL
- 24.8192 mL
- 5 mM
- 0.4964 mL
- 2.4819 mL
- 4.9638 mL
- 10 mM
- 0.2482 mL
- 1.2410 mL
- 2.4819 mL

技术信息

CAS号

130495-35-1

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H27ClN2O3

运输

蓝冰

分子量

402.91

别名

SKF 96365 (hydrochloride);SKF-96365;SKF-96,365

溶解度

DMSO	275.0 mg/mL (682.5 mM)
Water	290.0 mg/mL (719.8 mM)

动物实验配方

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1-(2-(4-Methoxyphenyl)-2-(3-(4-methoxyphenyl)propoxy)ethyl)-1H-imidazole hydrochloride Catalog No. CSN11934

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