- 产品描述: XEN907 is a potent and spirooxindole blocker of NaV1.7, with an IC50 of 3 nM. XEN907 also inhibits CYP3A4 in a recombinant human enzyme assay. XEN907 can be used for the research of pain
- 靶点: IC50: 3 nM (NaV1.7)
- 体外研究: 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
- 体内研究: XEN907 (10 mg/kg; p.o.) exhibits moderate oral bioavailability (13 %), Cmax (35 ng/mL), and AUClast (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
- 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.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.846 ml 14.229 ml 28.458 ml 5 mM 0.569 ml 2.846 ml 5.692 ml 10 mM 0.285 ml 1.423 ml 2.846 ml 50 mM 0.057 ml 0.285 ml 0.569 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)