ML402

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ML402 是 TREK-1 和 TREK-2 的激活剂，EC50 分别为 13.7 μM 和 5.9 μM。

ML402 is an activator of TREK-1 and TREK-2 with EC50s of 13.7 μM and 5.9 μM.(In Vitro):ML402 targets TRAAK with EC50 of 13.6 μM.

Xenopus oocyte two-electrode voltage-clamp measurements show that ML335 and ML402 activate K2P2.1 and K2P10.1 but not K2P4.1(14.3±2.7 μM, K2P2.1-ML335; 13.7±7.0 μM, K2P2.1-ML402; 5.2±0.5 μM, K2P10.1-ML335; and 5.9±1.6 μM, K2P10.1-ML402). The K2P modulator pocket has a single difference among TREK subfamily members at the cation-π interaction position, K2P2.1 Lys271, which is also a lysine in K2P10.1 but a glutamine in K2P4.1.Swapping the Lys271 equivalent between K2P2.1 and K2P4.1 results in a clear phenotype reversal for ML335 and M402 activation. K2P2.1 (K271Q) is insensitive to ML335 and ML402, whereas K2P4.1 (Q258K) responds to both with a similar EC50 to K2P2.1 (14.3±2.7 μM, K2P2.1-ML335; 16.2±3.0 μM, K2P4.1(Q258K)-ML335; 13.7±7.0 μM, K2P2.1-ML402; 13.6±1.5 μM, K2P4.1 (Q258K)-ML402) but with a lower magnitude response than K2P2.1.

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ZINC3671497 | N-[2-(4-chloro-2-methylphenoxy)ethyl]thiophene-2-carboxamide

Cell Cycle/DNA Damage

Potassium Channel

Estrogen Receptor/ERR

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298684-44-3

295.78

C14H14ClNO2S

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (338.09 mM)

Cc1cc(Cl)ccc1OCCNC(=O)c1cccs1

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(-20℃)

With Ice Pack

≥ 2 years