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GV-58 is a novel N- and P/Q-type calcium (Ca2+) channel agonist with EC50s of 7.21 and 8.81 μM, respectively. GV-58 slows the deactivation of channels, resulting in a large increase in presynaptic Ca2+ entry during activity. In 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.
| Molecular Weight | 374.5 |
| Formula | C18H26N6OS |
| CAS Number | 1402821-41-3 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Tyler B Tarr, et al. Synaptic Pathophysiology and Treatment of Lambert-Eaton Myasthenic Syndrome
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