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VU0810464 99%+

货号：A1219204 产品仅供科研

VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator,with EC50 of 720 nM for GIRK1/4 channels.

VU0810464 化学结构 CAS号：2126040-21-7
VU0810464 化学结构
CAS号：2126040-21-7
VU0810464 3D分子结构
CAS号：2126040-21-7
VU0810464 化学结构 CAS号：2126040-21-7
VU0810464 3D分子结构 CAS号：2126040-21-7
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VU0810464 纯度/质量文件

货号：A1219204 标准纯度：99%+
批次查询： 批次纯度:

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产品名称 Potassium Channel ↓ 其他靶点 纯度
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Glimepiride ++++

SUR2B, IC50: 7.3 nM

SUR1, IC50: 5.4 nM

 		97%
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Gliquidone ++

Potassium channel, IC50: 27.2 nM

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TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

 		99%+
Glibenclamide ✔ 98%
Amiodarone HCl ✔ 97%
Gliclazide ++

Potassium channel, IC50: 184 nM

 		98%
Repaglinide ✔ 98%
Dofetilide ✔ 98%
Nateglinide ✔ 99%
Quinine hydrochloride dihydrate ✔ 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

 		97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

VU0810464 生物活性

描述 G protein‐gated inwardly rectifying K+ (Kir3, also known as GIRK1) channels moderate the activity of excitable cells and have been implicated in neurological disorders and cardiac arrhythmias. Most neuronal Kir3 channels consist of Kir3.1 and Kir3.2 subtypes, while cardiac Kir3 channels consist of Kir3.1 and Kir3.4 subtypes. VU0810464 is a non-urea activator of Kir3.1/3.2 with nanomolar potency. It is >3‐fold more potent on Kir3.1/3.2‐expressing HEK‐293 cells compared to Kir3.1/3.4‐expressing cells in a TI+ flux assay. VU0810464 evoked a concentration‐dependent inward current in HPC (hippocampal) neurons from wild‐type mice, and this current was reversed by application of 0.3 mM Ba2+, which blocks inwardly rectifying K+ channels. Moreover, VU0810464 demonstrated a ~9‐fold higher potency for Kir3 channel activation in neurons as compared to SAN cells. Intraperitoneal dosing of a microsuspension of VU0810464 (30 mg/kg) revealed that it displayed a favourable distribution to the brain (unbound brain to plasma ratio, Kp,uu = 0.83). In male C57BL/6J mice, VU0810464 (0, 3, 10, and 30 mg/kg; i.p.) produced a dose‐dependent reduction of SIH (stress‐induced hyperthermia) response, without impacting baseline temperature[1].

VU0810464 参考文献

[1]Vo BN, Abney KK, Anderson A, et al. VU0810464, a non-urea G protein-gated inwardly rectifying K+ (Kir3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir3 channels and reduces stress-induced hyperthermia in mice. Br J Pharmacol. 2019;176(13):2238-2249

VU0810464 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.29mL

2.86mL

1.43mL

28.59mL

5.72mL

2.86mL

VU0810464 技术信息

CAS号2126040-21-7
分子式C18H21ClFN3O
分子量349.83
别名
运输蓝冰
存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 250 mg/mL(714.63 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: VU0810464 | 2126040-21-7 | VU 0810464 | VU-0810464 | GIRK Activator | Membrane Transporter/Ion Channel | Potassium Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | VU0810464 纯度/质量文件 | VU0810464 亚型比较 | VU0810464 生物活性 | VU0810464 参考文献 | VU0810464 实验方案 | VU0810464 技术信息

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