Identification | Back Directory | [Name]
XEN907 | [CAS]
912656-34-9 | [Synonyms]
XEN907 XEN907; XEN 907; XEN-907 1'-pentylspiro[6H-furo[2,3-f][1,3]benzodioxole-7,3'-indole]-2'-one Spiro[furo[2,3-f]-1,3-benzodioxole-7(6H),3'-[3H]indol]-2'(1'H)-one, 1'-pentyl- 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 | [Molecular Formula]
C21H21NO4 | [MDL Number]
MFCD25371548 | [MOL File]
912656-34-9.mol | [Molecular Weight]
351.4 |
Chemical Properties | Back Directory | [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 | [form ]
Solid | [pka]
-0.19±0.20(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [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. |
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Company Name: |
Musechem
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Tel: |
+1-800-259-7612 |
Website: |
www.musechem.com |
Company Name: |
Wuhan Topule
|
Tel: |
+86-02787215551 +86-19945035818 |
Website: |
http://www.topule.com/ |
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