XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor with an IC50 of 41 nM for hNaV1.6. It also potently blocks NaV1.2 with an IC50 of 125 nM and demonstrates anticonvulsant activity. It shows high selectivity over NaV1.1 and NaV1.5. Additionally, XPC-6444 exhibits good metabolic stability in human liver microsomes and hepatocytes, and a low potential for MDR1 mediated efflux.
- Highly potent, isoform-selective, and CNS-penetrant Nav1.6 inhibitor
- Potently blocks Nav1.2
- Demonstrates anticonvulsant activity
- Shows high selectivity over Nav1.1 and Nav1.5
- Exhibits good metabolic stability in human liver microsomes and hepatocytes
- Low potential for MDR1 mediated efflux