For research use only. Not for therapeutic Use.
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].
| Catalog Number | I017825 |
| CAS Number | 2230144-21-3 |
| Synonyms | 4-[[2-[[tert-butyl(methyl)amino]methyl]-6-fluorophenyl]methylamino]-2,6-difluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide |
| Molecular Formula | C22H25F3N4O2S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H25F3N4O2S2/c1-22(2,3)29(4)11-14-6-5-7-17(23)16(14)10-26-15-8-18(24)21(19(25)9-15)33(30,31)28-20-12-32-13-27-20/h5-9,12-13,26,28H,10-11H2,1-4H3 |
| InChIKey | VOJFVKGTRNXOTJ-UHFFFAOYSA-N |
| SMILES | CC(C)(C)N(C)CC1=C(C(=CC=C1)F)CNC2=CC(=C(C(=C2)F)S(=O)(=O)NC3=CSC=N3)F |
| Reference | [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. |
