XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant Na V 1.6 inhibitor ( IC 50 =41 nM for hNa V 1.6). XPC-6444 also displays potent block of Na V 1.2 (IC 50 =125 nM). XPC-6444 shows anticonvulsant activity
In Vitro
XPC-6444 shows high selectivity over Na V 1.1 and Na V 1.5. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
XPC-6444 exhibits good metabolic stability in human liver microsomes and hepatocytes, and low potential for MDR1 mediated efflux . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:IC50: 41 nM (hNa V 1.6), 125 nM (hNa V 1.2)