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CAS No.: 1333210-07-3

SAR7334 Catalog No. CSN18783

Synonyms: CPA-1588

SAR7334 is a potent TRPC6 (Transient receptor potential cation channel, subfamily C, member 6) inhibitor.

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400-920-2911

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实验方案

技术信息

生物活性

描述The cation channel transient receptor potential canonical (TRPC) 6 has been associated with several pathologies including focal segmental glomerulosclerosis, pulmonary hypertension and ischaemia reperfusion-induced lung oedema. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca²⁺ influx into cells with IC₅₀s of 9.5, 282 and 226 nM. SAR7334 dose-dependently reduces TRPC6 currents with an IC₅₀ of 7.9 nM. In most TRPC6-HEK-FITR cells, trypsin evoked large, rapidly declining TRPC6 currents that reached an almost steady-state level within 30–60 s. This current was substantially reduced by 100 nM SAR7334. The reduction of trypsin-induced TRPC6 currents by 100 nM SAR7334 amounted to 88 ± 3% (n = 5). In perfused isolated lungs from mice, SAR7334 abolished hypoxia-induced increases in pulmonary arterial pressure. Half maximal inhibition was achieved at about 100 nM indicating that SAR7334 is able to efficiently block native TRPC6 channels in situ^[3].
参考文献

[1] Ilatovskaya DV, Palygin O, et al. The Role of Angiotensin II in Glomerular Volume Dynamics and Podocyte Calcium Handling. Sci Rep. 2017 Mar 22;7(1):299.
[2] Maier T, Follmann M, et al. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol. 2015 Jul;172(14):3650-60.
[3] Maier T, Follmann M, Hessler G, et al. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol. 2015;172(14):3650‐3660

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
- 2.7183 mL
- 13.5917 mL
- 27.1834 mL
- 5 mM
- 0.5437 mL
- 2.7183 mL
- 5.4367 mL
- 10 mM
- 0.2718 mL
- 1.3592 mL
- 2.7183 mL

技术信息

CAS号

1333210-07-3

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H22ClN3O

运输

蓝冰

分子量

367.87

别名

CPA-1588

溶解度

DMSO	74.0 mg/mL (201.2 mM)
Water	Insoluble
Ethanol	73.0 mg/mL (198.4 mM)

动物实验配方

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