CAS NO: | 1402821-41-3 |
规格: | 98% |
分子量: | 374.5 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
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.