ICA 121431 is a synthetic potent and selective inhibitor of human NaV1.3 and NaV1.1 channels. ICA 121431 has an effective concentration of 10nM - 1μM with an IC50 of 13 and 23 nM on the NaV1.3 and NaV1.1 channels respectively. Unlike other known NaV inhibitors ICA inhibits the Nav channel by interacting with the S1-S4 voltage sensor segment of homologous domain 4. The sensitivity and selectivity of different NaV subtype receptors to ICA is influenced by the extracellular amino acid residues in the facing regions of the S2 and S3 transmembrane segments. Currently, most NaV modulators are unable to distinguish between NaV channel subtypes therefore limiting their usage due to systemic toxicity. ICA’s interaction with the region of the channel that controls voltage sensitivity enables subtype selective modulation and may be used as an efficient tool for innovative drug development
产品描述
A Potent and Selective Blocker of NaV1.3 and NaV1.1 Channels
