kv7.2

XE991 是一种新型具有选择性的 Kv7 (KCNQ)通道阻滞剂。XE 991 抑制 Kv7.1 (KCNQ1)、Kv7.2 (KCNQ2)、Kv7.2 + Kv7.3 (KCNQ3)通道及M-current，可用于研究神经系统疾病。

KCNQ2 3 activator-1 是Kv7.2 Kv7.3(KCNQ2 3) 钾通道激活剂，详细信息来自专利 WO2021113757A1的化合物 A。

Kv7.2 modulator 1 (compound 10) 作为Kv7.2 channel的调节剂，适用于癫痫研究领域。

Kv7.2 modulator 2 (compound 52) 作为Kv7.2 channel的调制剂，主要应用于癫痫的研究领域。

Kv7.2 Kv7.3 activator-1 (compound 517) 作为一种高效的Kv7.2 Kv7.3通道激活剂，其激活效力(EC50)低于1 µM。该化合物对于神经系统疾病的研究展示了极大的应用潜力。

Kv7.2 Kv7.3 agonist 1 (Compound 16) 作为一种口服激动剂，针对KV7.2 7.3通道（KV7.2 7.3 channel KCNQ2 3），其EC50值为1.03 μM。在实验动物模型中，该化合物在小鼠的慢性压迫性损伤（CCI）和Streptozotocin诱导的糖尿病周围神经性疼痛（DPNP）模型中具有显著的镇痛效果，ED50值分别达到12.02和9.63 mg kg。

ZTZ240 是一种 KCNQ2 通道激活剂，可用于研究癫痫。

ICA-105665 (PF-04895162) 是一种有效的口服活性的神经元 Kv7.2 7.3和 Kv7.3 7.5钾通道激动剂。ICA-105665 在人肝细胞中具有低细胞毒性潜力，但抑制肝线粒体功能和胆盐输出蛋白 (BSEP) 转运 (IC50为 311 μM)。ICA-105665 可穿透中枢神经系统 (CNS)并具有抗癫痫作用。

XE 991 dihydrochloride 是有效的 Kv7 (KCNQ)通道阻滞剂，抑制 Kv7.1 (KCNQ1)，Kv7.2 (KCNQ2)，Kv7.2 + Kv7.3 (KCNQ3)通道以及 M-current，IC50分别为 0.75 µM、0.71 µM、0.6 μM、0.98 µM。

QO-58 is a Kv7 channel opener with EC50 values of 7.0, 1.0, 5.2, 0.6 μM for Kv7.1, Kv7.2, Kv7.3 7.5, Kv7.4 respectively. QO-58 increases the pain threshold of neuropathic pain in a sciatic nerve CCI in vivo.

ML213 (CID-3111211) 是有效的、选择性的Kv7.2和Kv7.4通道增强剂，EC50值分别为 230 nM 和 510 nM。

ML252是一种钾离子通道(potassium channel)的选择性抑制剂，主要针对KCNQ2 (Kv7.2，IC50=69 nM)。同时，ML252对细胞色素Cytochrome P450也有抑制作用，其IC50值分别为CYP1A2为6.1 nM、CYP2C9为18.9 nM、CYP3A4为3.9 nM、CYP2D6为19.9 nM。

PF05020182 is novel potent and selective Kv7.2 4 potassium channel opener. PF-05020182 (2) significantly inhibits convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 support further development as an adjunctive treatment of refractory epilepsy. Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in controlling spontaneous electrical activity during epileptic seizures.

ML-252 is a potent, selective inhibitor of the Kv7.2 voltage-gated potassium channel, demonstrating an IC50 value of 69 nM in patch clamp assays. It exists as the (S)-enantiomer, which is significantly more effective than both its (R)-enantiomer counterpart and the racemic mixture, with respective IC50 values of 944 nM and 160 nM. ML-252 exhibits high selectivity for Kv7.2 over other potassium channel subtypes and shows minimal activity against more than 68 G protein-coupled receptors, various transporters, L- and N-type calcium channels, K_ATP, and hERG potassium channels. However, it does inhibit the melatonin MT1 receptor by 61% at a 10 µM concentration.