2230144-21-3

XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 also displays potent block of NaV1.2 (IC50=125 nM). XPC-6444 shows anticonvulsant activity[1]. XPC-6444 shows high selectivity over NaV1.1 and NaV1.5[1]. XPC-6444 exhibits good metabolic stability in human liver microsomes and hepatocytes, and low potential for MDR1 mediated efflux[1].

[1]. Focken T, et al. Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective NaV1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy. J Med Chem. 2019 Oct 3.