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ML 418 是第一个有效的、选择性的和 CNS 穿透性的 Kir7.1 钾通道 (IC50, 310 nM) 阻断剂,它也有效地抑制 Kir6.2/SUR1,并且表现出优于其他 Kir 通道的选择性。
Kir7.1 inhibitor (IC50 = 0.31 μM). Also inhibits Kir6.2 with similar potency. Displays >17-fold selectivity for Kir7.1 over Kir1.1, Kir2.1, Kir2.2, Kir2.3, Kir3.1/3.2 and Kir4.1. Active in vivo.
Swale et al (2016) ML418: the first selective, sub-micromolar pore blocker of Kir7.1 potassium channels. ACS Chem.Neurosci. 7 1013 PMID:27184474 |Kharade (2017) Pore polarity and charge determine differential block of Kir1.1 and Kir7.1 potassium channels by small-molecule inhibitor VU590. Mol.Pharmacol. 92 338 PMID:28619748
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