| Bioactivity | 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[1][2]. | ||||||||||||
| Target | IC50: 3 nM (NaV1.7) | ||||||||||||
| Invitro | XEN907 is not cytotoxic in HepG2 cells (% viable after 16 h: >99%)[1].XEN907 shows moderate hepatocyte stability (% remaining after 2 h: rat 21%; human 34%; dog 46%) across species[1]. | ||||||||||||
| In Vivo | XEN907 (10 mg/kg; p.o.) exhibits moderate oral bioavailability (13 %), Cmax (35 ng/mL), and AUClast (143 h•ng/mL) in rats[1].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[1]. | ||||||||||||
| Name | XEN907 | ||||||||||||
| CAS | 912656-34-9 | ||||||||||||
| Formula | C21H21NO4 | ||||||||||||
| Molar Mass | 351.40 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |