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CAS No. : 1052515-91-9
MCE 国际站:VU0134992 hydrochloride
产品活性: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。
研究领域:Membrane Transporter/Ion Channel
作用靶点:Potassium Channel
In Vitro: VU0134992 hydrochloride is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2, is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1, and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2.The selectivity of VU0134992 hydrochloride for Kir4.1 versus nine other members of the Kir channel family was evaluated at concentrations ranging from 0.3 nM to 30 µM in 11-point CRC experiments, using established Tl+ flux assays. VU0134992 hydrochloride inhibits Kir3.1/Kir3.2 (92% inhibition at 30 µM, IC50=2.5 µM), Kir3.1/Kir3.4 (92% inhibition at 30 µM, IC50=3.1 µM), and Kir4.2 (100% inhibition at 30 µM, IC50=8.1 µM) with approximately the same efficacy and potency that VU0134992 inhibits Kir4.1 (100% at 30 µM, IC50=5.2 µM).
In Vivo: VU0134992 hydrochloride (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na+ as well as K+ excretion.
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