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GV-58
本半岛bd体育手机客户端 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。
GV-58图片
CAS NO: 1402821-41-3
包装与价格：
包装 价格(元)
10mM (in 1mL DMSO) 电议
1mg 电议
5mg 电议

半岛bd体育手机客户端 介绍
GV-58是N-和P/Q-type钙离子通道激动剂，EC50值分别为7.21和8.81uM，对CDK类激酶的抑制作用弱20倍，是(R)-roscovitine的优化化合物。
Cas No. 1402821-41-3
别名 (2R)-2-[[6-[[(5-甲基噻吩-2-基)甲基]氨基]-9-丙基-9H-嘌呤-2-基]氨基]丁烷-1-醇
Canonical SMILES CC[C@@H](NC1=NC(NCC2=CC=C(C)S2)=C3N=CN(CCC)C3=N1)CO
分子式 C18H26N6OS
分子量 374.5
溶解度 DMSO : 50 mg/mL (133.51 mM);Water :< 0.1 mg/mL (insoluble)
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.IC50 value: 7.21/8.81 uM (N-type/P-Q-type Ca2+ channel) [1]Target: Ca2+ channel agonistIn comparison with the parent molecule, (R)-roscovitine, GV-58 has a 20-fold less potent cyclin-dependent kinase antagonist effect, a 3- to 4-fold more potent Ca2+ channel agonist effect, and 4-fold higher efficacy as a Ca2+ channel agonist. GV-58 had no agonist activity (up to 100 μm) on the L-type α-subunit we tested (Cav1.3). In summary, GV-58 greatly improved upon (R)-roscovitine in terms of our properties of interest, with a ～4-fold increase in efficacy as an agonist for N- and P/Q-type Ca2+ channels, a ～3- to 4-fold increase in potency as an agonist for N- and P/Q-type Ca2+ channels, and a 20-fold decrease in potency as a Cdk antagonist.

[1]. Tarr TB, et al. Evaluation of a novel calcium channel agonist for therapeutic potential in Lambert-Eaton myasthenic syndrome. J Neurosci. 2013 Jun 19;33(25):10559-67.
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