XPC-6444 是一种高效的，亚型选择性的，CNS-渗透性的 NaV1.6 抑制剂 (对 hNaV1.6 的IC50=41 nM)。XPC-6444 也有效阻断了 NaV1.2 (IC50=125 nM)。XPC-6444 具有抗惊厥活性。
货号:ajcx35334
CAS:2230144-21-3
分子式:C22H25F3N4O2S2
分子量：498.58
溶解度:DMSO : 125 mg/mL (250.71 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.