XEN907
XEN907 Basic information
- Product Name:
- XEN907
- Synonyms:
-
- XEN907
- 1-CYCLOPENTYL-1,2-DIHYDRO-6',10',12'-TRIOXASPIRO[INDOLE-3,4'-TRICYCLO[7.3.0.0^{3,7}]DODECANE]-1',3'(7'),8'-TRIEN-2-ONE
- XEN907; XEN 907; XEN-907
- Spiro[furo[2,3-f]-1,3-benzodioxole-7(6H),3'-[3H]indol]-2'(1'H)-one, 1'-pentyl-
- 1'-pentylspiro[6H-furo[2,3-f][1,3]benzodioxole-7,3'-indole]-2'-one
- XEN907,XEN-907
- 1-Pentyl-6'H-spiro[indoline-3,7'-[1,3]dioxolo[4,5-f]benzofuran]-2-one
- XEN907, 10 mM in DMSO
- CAS:
- 912656-34-9
- MF:
- C21H21NO4
- MW:
- 351.4
- Mol File:
- 912656-34-9.mol
XEN907 Chemical Properties
- Melting point:
- 88-90 °C
- Boiling point:
- 566.9±50.0 °C(Predicted)
- Density
- 1.34±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- -0.19±0.20(Predicted)
- form
- Solid
- color
- White to off-white
XEN907 Usage And Synthesis
Description
XEN907 is a novel spirooxindole NaV1.7 blocker with IC50 of 3 nM. It shows a further 10-fold increase in potency, which represents a promising structure for further optimization efforts in vitro.
Uses
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].
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].
IC 50
Nav1.7
References
[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. DOI:10.1016/j.bmcl.2011.04.088
[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.
XEN907Supplier
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