|N-(2-(4-氯-2-甲基苯氧基)乙基)噻吩-2-甲酰胺|CsnPharm

CAS No.: 298684-44-3

ML402 Catalog No. CSN20652

Synonyms: ML402

ML402 is a selective TREK-1 activator.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Polymodal thermo- and mechanosensitive two-pore domain potassium (K_2P) channels of the TREK subfamily generate 'leak' currents that regulate neuronal excitability, respond to lipids, temperature and mechanical stretch, and influence pain, temperature perception and anaesthetic responses. In contrast to other potassium channels, K_2P channels use a selectivity filter 'C-type' gate as the principal gating site. ML402 is a selective small-molecule K_2P2.1 (also known as TREK-1) activator. Xenopus oocyte two electrode voltage-clamp measurements show that ML402 activates K_2P2.1(TREK-1) and K_2P10.1(TREK-2) but not K_2P4.1(TRAAK) (13.7± 7.0 μM, K_2P2.1(TREK-1); and 5.9 ± 1.6 μM, K_2P10.1(TREK-2)). ML402 activates K_2P2.1(TREK-1) in HEK293 cells similar to its effects in Xenopus oocytes (5.9 ± 1.6 μM, (n≥3)) ^[2].
作用机制ML402 adopts an L-shaped conformation enabling its ‘upper ring’ (thiophene) and ‘lower ring’ (aryl ether) to engage the P1 helix residue Phe134 through face-face and edge-face interactions ^[2].
参考文献

[1] Lolicato M, Arrigoni C, et al. K(2P)2.1 (TREK-1)-activator complexes reveal a cryptic selectivity filter binding site. Nature. 2017 Jul 20;547(7663):364-368.
[2] Lolicato M, Arrigoni C, Mori T, Sekioka Y, Bryant C, Clark KA, Minor DL Jr. K2P2.1 (TREK-1)-activator complexes reveal a cryptic selectivity filter binding site. Nature. 2017 Jul 20;547(7663):364-368. doi: 10.1038/nature22988. Epub 2017 Jul 10. PMID: 28693035; PMCID: PMC5778891.

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
- 3.3808 mL
- 16.9042 mL
- 33.8084 mL
- 5 mM
- 0.6762 mL
- 3.3808 mL
- 6.7617 mL
- 10 mM
- 0.3381 mL
- 1.6904 mL
- 3.3808 mL

技术信息

CAS号

298684-44-3

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H14ClNO2S

运输

蓝冰

分子量

295.78

别名

ML402

溶解度

DMSO	100.0 mg/mL (338.1 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

ML402 Catalog No. CSN20652

靶点选择性

请登录您的专属账户

确认信息