Ceratotoxin-1 (β-theraphotoxin-Cm1a, β-TRTX-Cm1a, CcoTx1) is a NaV channel blocker. This peptide toxin was originally isolated from the spider species Ceratogyrus marshalli (Straighthorned baboon tarantula). The toxin binds to all NaV channels in the central nervous system apart from NaV1.3. Mice injected with 500 pmol of Ceratotoxin-1 exhibited symptoms of neurological toxicity in the form of difficulty of standing, breathing reduction and flaccid paralysis. Ceratotoxin-1 also decreases Na+ influx in NaV1.1, NaV1.2, NaV1.4. It is especially selective for NaV1.2 with an IC50 value of 3±1 nM.
产品描述
A Blocker of NaV channels
产品形式
There are currently nine types of voltage-gated Na+ (NaV) channels defined and characterized. The channels are responsible for propagation and the creation of action potential in excitable cells. The channel is comprised of the main α subunit and the β auxiliary subunits. Although the α subunit is sufficient for channel expression it is the β subunit that modifies the kinetics and voltage dependency of the channel. The α subunits are organized in four homologous domains (I-IV) each containing six transmembrane α helices (S1-S6).
