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Linopirdine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Linopirdine图片
CAS NO:105431-72-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
Linopirdine (DuP 996) 是一种具有口服活性的选择性 M 型 K+ current (IM; Kv7; KCNQ Channels) 抑制剂,IC50 为 2.4 μM。
Cas No.105431-72-9
别名利诺吡啶,DuP 996
Canonical SMILESO=C1C(CC2=CC=NC=C2)(CC3=CC=NC=C3)C4=CC=CC=C4N1C5=CC=CC=C5
分子式C26H21N3O
分子量391.5
溶解度DMF: 30 mg/mL,DMSO: 25 mg/mL,Ethanol: 30 mg/mL,Ethanol:PBS (pH 7.2) (1:30): 0.03 mg/mL
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Linopirdine is an enhancer of the stimulus-evoked but not basal release of several neurotransmitters, including acetylcholine, dopamine, serotonin, and glutamate. It increases acetylcholine release in rat hippocampal CA1 neurons by blocking voltage-gated, calcium-activated and leak (M-type; Kv7.2/7.3; KCNQ2/3) K+ current with an IC50 value of 2.4 µM. Inhibition of M-channels is reported to result in the depolarization of CA3 pyramidal neurons and activated presynaptic voltage-gated P/Q- and N-type calcium channels, which leads to Ca2+ influx and increased neurotransmitter release. Linopirdine has been shown to produce a number of effects including EEG patterns of enhanced vigilance, induction of c-fos expression in cerebral cortex, reduction of the increase of cerebral glucose utilization induced by hypoxia, and improved performance in animal models of learning and memory. Linopirdine has also been identified as an agonist of transient receptor potential vanilloid type 1 (EC50 = 115 µM in HEK293 cells voltage clamped at -60 mV).