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VU0134992 hydrochloride

CAS No. : 1052515-91-9

MCE 站：VU0134992 hydrochloride

产品活性：VU0134992 hydrochloride 是个亚型偏好的，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 ?M in 11-point CRC experiments, using established Tl+ flux assays. VU0134992 hydrochloride inhibits Kir3.1/Kir3.2 (92% inhibition at 30 ?M, IC₅₀=2.5 ?M), Kir3.1/Kir3.4 (92% inhibition at 30 ?M, IC₅₀=3.1 ?M), and Kir4.2 (100% inhibition at 30 ?M, IC₅₀=8.1 ?M) with approximately the same efficacy and potency that VU0134992 inhibits Kir4.1 (100% at 30 ?M, IC₅₀=5.2 ?M).

In Vivo: VU0134992 hydrochloride (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na⁺ as well as K⁺ excretion.

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