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GV-58
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。
GV-58图片
CAS NO:1402821-41-3
规格:98%
分子量:374.5
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
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:1402821-41-3
分子式:C18H26N6OS
分子量:374.5
纯度:98%
存储:Store at -20°C

Background:

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.