产品
编 号：F449940
分子式：C20H31BrN2O2
分子量：411.38
分子式：C20H31BrN2O2
分子量：411.38
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CAS No: 755002-90-5
产品详情
生物活性：
VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 μM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 μM) at -120 mV.
体内研究：
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
体外研究：
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 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 μM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 μM) at -120 mV.
体内研究：
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
体外研究：
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).
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