XEN907 is a potent and spirooxindole blocker of Na V 1.7, with an IC 50 of 3 nM. XEN907 also inhibits CYP3A4 in a recombinant human enzyme assay. XEN907 can be used for the research of pain.
性状
Solid
IC50 & Target[1][2]
IC50: 3 nM (NaV1.7)
体外研究(In Vitro)
XEN907 is not cytotoxic in HepG2 cells (% viable after 16 h: >99%).XEN907 shows moderate hepatocyte stability (% remaining after 2 h: rat 21%; human 34%; dog 46%) across species. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
XEN907 (10 mg/kg; p.o.) exhibits moderate oral bioavailability (13 %), C max (35 ng/mL), and AUC last (143 h?ng/mL) in rats.
XEN907 (3 mg/kg; i.v.) exhibits terminal elimination half-life (2.6 h), high plasma clearance (9.4 L/h/kg), and large volumes of distribution (35.0 L/kg) in rats. 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]. Chowdhury S, et al. Discovery of XEN907, a spirooxindole blocker of NaV1.7 for the treatment of pain. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3676-81.[2]. Chowdhury S, et, al. Tetracyclic spirooxindole blockers of hNaV1.7: activity in vitro and in CFA-induced inflammatory pain model. Med Chem Res (2013) 22:1825–1836.
溶解度数据
In Vitro: DMSO : 100 mg/mL (284.58 mM; Need ultrasonic)配制储备液