GV-58, a Ca2+ channel agonist, is selective for N- (CaV2.2) and P/Q-type (CaV2.1) channels. GV-58 was developed as a modification of (R)-roscovitine, which was previously shown to be a Ca2+ channel agonist. 100 μM GV-58 was originally tested on N-, P/Q-, or L-type channels expressed in tsA-201 cells. GV-58 was shown to be more potent on N- and P/Q Ca2+ channels with an EC50 = 6.8 and 9.9 μM, respectively over L-type calcium channels (EC50 > 100 μM)1. GV-58 slows the closing of the channel, resulting in a large increase in total Ca2+ entry during motor nerve action potential activity.
产品描述
An Activator of CaV2.2 and CaV2.1 Ca2+ Channels
产品形式
GV-58, a Ca2+ channel agonist, is selective for N- (CaV2.2) and P/Q-type (CaV2.1) channels. GV-58 was developed as a modification of (R)-roscovitine, which was previously shown to be a Ca2+ channel agonist. 100 μM GV-58 was originally tested on N-, P/Q-, or L-type channels expressed in tsA-201 cells. GV-58 was shown to be more potent on N- and P/Q Ca2+ channels with an EC50 = 6.8 and 9.9 μM, respectively over L-type calcium channels (EC50 > 100 μM)1. GV-58 slows the closing of the channel, resulting in a large increase in total Ca2+ entry during motor nerve action potential activity.