SNX-482 is a peptidyl toxin originally isolated from venom of the spider Hysterocrates gigas. Native SNX-482 blocks specifically CaV2.3 (α1E, R-type) channels in a voltage dependent manner. The block is reversible only upon application of strong voltage to facilitate unbinding.2 SNX-482 inhibits human CaV2.3 channels stably expressed in a mammalian cell line. An IC50 of 15-30 nM was obtained for block of Cav2.3 channel, using either patch clamp electrophysiology or K+-evoked Ca2+ flux. At low nanomolar concentrations, SNX-482 also blocked a native R-type Ca2+ current in rat neurohypophyseal nerve terminals, but concentrations of 200-500 nM had no effect on R-type Ca2+ currents in several types of rat central neurons. SNX-482 was also used to demonstrate the contribution of CaV2.3 channels to transmitter release. Recently it was shown that higher concentrations of SNX-482 also block CaV2.1 channels in chromaffin cells.
产品描述
A Blocker of R-Type Ca2+ (CaV2.3) and A-Type (KV4.2, KV4.3) K+ Channels
产品形式
SNX-482 is a peptidyl toxin originally isolated from venom of the spider Hysterocrates gigas. Native SNX-482 blocks specifically CaV2.3 (α1E, R-type) channels in a voltage dependent manner. The block is reversible only upon application of strong voltage to facilitate unbinding.2 SNX-482 inhibits human CaV2.3 channels stably expressed in a mammalian cell line. An IC50 of 15-30 nM was obtained for block of Cav2.3 channel, using either patch clamp electrophysiology or K+-evoked Ca2+ flux. At low nanomolar concentrations, SNX-482 also blocked a native R-type Ca2+ current in rat neurohypophyseal nerve terminals, but concentrations of 200-500 nM had no effect on R-type Ca2+ currents in several types of rat central neurons. SNX-482 was also used to demonstrate the contribution of CaV2.3 channels to transmitter release. Recently it was shown that higher concentrations of SNX-482 also block CaV2.1 channels in chromaffin cells.