| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 41 nM (hNaV1.6), 125 nM (hNaV1.2) | ||||||||||||
| Invitro | XPC-6444 shows high selectivity over NaV1.1 and NaV1.5[1]. | ||||||||||||
| In Vivo | XPC-6444 exhibits good metabolic stability in human liver microsomes and hepatocytes, and low potential for MDR1 mediated efflux[1]. | ||||||||||||
| Name | XPC-6444 | ||||||||||||
| CAS | 2230144-21-3 | ||||||||||||
| Formula | C22H25F3N4O2S2 | ||||||||||||
| Molar Mass | 498.58 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |
XPC-6444
CAS: 2230144-21-3 F: C22H25F3N4O2S2 W: 498.58
XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 al
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