产品
编 号：F548368
分子式：C20H32BrClN2O2
分子量：447.84
分子式：C20H32BrClN2O2
分子量：447.84
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1052515-91-9
产品详情
生物活性：
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 μM. VU0134992 hydrochloride 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 hydrochloride (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:Oral gavage
Administration:50 and 100 mg/kg
Result:Statistically significantly increased urinary Na+ as well as K+ excretion.
体外研究：
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).
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 μM. VU0134992 hydrochloride 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 hydrochloride (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:Oral gavage
Administration:50 and 100 mg/kg
Result:Statistically significantly increased urinary Na+ as well as K+ excretion.
体外研究：
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).
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