VU 0134992

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VU0134992 是一种 Kir4.1 阻断剂，IC50 值为 0.97 μM。

VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM.

VU0134992 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 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 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).

VU0134992 (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na+ as well as K+ excretion. Animal Model:Male Sprague-Dawley rats (250-300 g)Dosage:50 and 100 mg/kg Administration:Oral gavage Result:Statistically significantly increased urinary Na+ as well as K+ excretion

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Cell Cycle/DNA Damage

Potassium Channel

Kir4.1

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755002-90-5

411.38

C20H31BrN2O2

>98% (HPLC)

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CC(C)c1ccc(OCC(=O)NC2CC(C)(C)NC(C)(C)C2)c(Br)c1

2-(2-Bromo-4-isopropylphenoxy)-N-(2266-tetramethylpiperidin-4-yl)acetamide

(-20℃)

With Ice Pack

≥ 2 years