|2-((5-氯喹啉-8-基)氧基)-N,N-二乙基乙胺二盐酸盐|CsnPharm

CAS No.: 861038-72-4

A2764 2HCl/A2764二盐酸盐 Catalog No. CSN25279

Synonyms: A2764 (hydrochloride)

A2764 dihydrochloride is a selective inhibitor of TRESK (KCNK18) with an IC50 value of 11.8 μM. A2764 can inhibit TRESK in native cells, leading to cell depolarization and increased excitability.

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技术信息

生物活性

描述A2764 2HCl is a highly selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception. The degree of inhibition by 100 µM A2764 (77.8% ± 3.5%, n = 6) was larger in the activated state of TRESK (i.e., after calcineurin-dependent stimulation) than in the resting state of the channel (42.8% ± 11.5% inhibition, n = 7). A2764 (100 µM) shows an improved inhibitory potency for activated channel. The subsequent application of A2764 strongly inhibits the current (77.8±3.5%)^[1].
参考文献

[1] Lengyel M, Erdélyi F, Pergel E, et al. Chemically Modified Derivatives of the Activator Compound Cloxyquin Exert Inhibitory Effect on TRESK (K2P18.1) Background Potassium Channel. Mol Pharmacol. 2019;95(6):652-660

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
- 2.8433 mL
- 14.2167 mL
- 28.4334 mL
- 5 mM
- 0.5687 mL
- 2.8433 mL
- 5.6867 mL
- 10 mM
- 0.2843 mL
- 1.4217 mL
- 2.8433 mL

技术信息

CAS号

861038-72-4

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H21Cl3N2O

运输

蓝冰

分子量

351.70

别名

A2764 (hydrochloride)

溶解度

DMSO	68.0 mg/mL (193.3 mM)
Ethanol	69.0 mg/mL (196.2 mM)

动物实验配方

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A2764 2HCl/A2764二盐酸盐 Catalog No. CSN25279

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