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.
性状
Solid
IC50 & Target[1][2]
IC50: 41 nM (hNaV1.6), 125 nM (hNaV1.2)
体外研究(In Vitro)
XPC-6444 shows high selectivity over NaV1.1 and NaV1.5. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
XPC-6444 exhibits good metabolic stability in human liver microsomes and hepatocytes, and low potential for MDR1 mediated efflux. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 125 mg/mL (250.71 mM; Need ultrasonic)配制储备液