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VU0134992 hydrochloride 是第一个亚型偏好的,具有口服活性和选择性的内向整流钾通道 Kir4.1 阻滞剂,IC50 值为 0.97 μM。VU0134992 hydrochloride 在 -120 mV 时,对同分 Kir4.1 比 Kir4.1/5.1 共分通道 (IC50=9 μM) 高出 9 倍的选择性。
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV[1].
[1]. Kharade SV, et al. Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992. Mol Pharmacol. 2018 Aug;94(2):926-937.
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