1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. VU0134992

VU0134992 是第一个亚型偏好的,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 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。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 VU0134992 hydrochloride 通常具有更好的水溶性和稳定性。

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VU0134992 Chemical Structure

VU0134992 Chemical Structure

CAS No. : 755002-90-5

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  • 生物活性

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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[1].

IC50 & Target

IC50: 0.97 µM (Kir4.1)[1]

体外研究
(In Vitro)

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[1]. 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)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

VU0134992 (50-100 mg/kg; oral gavage) statistically significantly increased urinary Na+ as well as K+ excretion[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (250-300 g)[1]
Dosage: 50 and 100 mg/kg
Administration: Oral gavage
Result: Statistically significantly increased urinary Na+ as well as K+ excretion
分子量

411.38

Formula

C20H31BrN2O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
VU0134992
目录号:
HY-122560
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