CAS:2126040-21-72-(3-Chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide

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VU0810464 2-(3-氯-4-氟苯基)-N-(1-环己基-3-甲基-1H-吡唑-5-基)乙酰胺 Cat No. FB16491Cas No. 2126040-21-7

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.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8585 mL
- 14.2926 mL
- 28.5853 mL
- 5 mM
- 0.5717 mL
- 2.8585 mL
- 5.7171 mL
- 10 mM
- 0.2859 mL
- 1.4293 mL
- 2.8585 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

2126040-21-7

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C18H21ClFN3O

运输

蓝冰

分子量

349.83

别名

溶解度

DMSO	250.0 mg/mL (714.6 mM)

动物实验配方

靶点数据

生物活性

描述G protein‐gated inwardly rectifying K⁺ (K_ir3, also known as GIRK1) channels moderate the activity of excitable cells and have been implicated in neurological disorders and cardiac arrhythmias. Most neuronal K_ir3 channels consist of K_ir3.1 and K_ir3.2 subtypes, while cardiac K_ir3 channels consist of K_ir3.1 and K_ir3.4 subtypes. VU0810464 is a non-urea activator of K_ir3.1/3.2 with nanomolar potency. It is >3‐fold more potent on K_ir3.1/3.2‐expressing HEK‐293 cells compared to K_ir3.1/3.4‐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 K_ir3 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, K_p,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].