CAS:298684-44-3ML402

ML402 is a selective TREK-1 activator.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

298684-44-3

储存条件

分子式

C14H14ClNO2S

运输

蓝冰

分子量

295.78

别名

溶解度

DMSO	100.0 mg/mL (338.1 mM)

动物实验配方

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)) .
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 .