2126040-21-7|2-(3-Chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide|CsnPharm

CAS No.: 2126040-21-7

VU0810464 Catalog No. CSN25285

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.

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技术信息

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].
参考文献

[1] Vo BN, Abney KK, Anderson A, et al. VU0810464, a non-urea G protein-gated inwardly rectifying K⁺ (K_ir3/GIRK) channel activator, exhibits enhanced selectivity for neuronal K_ir3 channels and reduces stress-induced hyperthermia in mice. Br J Pharmacol. 2019;176(13):2238-2249

实验方案

计算器摩尔计算器总药量计算器工作液计算器
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

技术信息

CAS号

2126040-21-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -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

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