VU 0134992

Research use only, not for human use.

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