XEN907
目录号: PL11342 纯度: ≥98%
CAS No. :912656-34-9
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中文名称
XEN907
中文别名
XEN907
英文名称
XEN907
英文别名
XEN 907;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;XEN-907;XEN907;1′-Pentylspiro[furo[2,3-f]-1,3-benzodioxole-7(6H),3′-[3H]indol]-2′(1′H)-one (ACI)
Cas No.
912656-34-9
分子式
C21H21NO4
分子量
351.40
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
XEN907 是一种有效的螺羟吲哚类 NaV1.7 阻滞剂,IC50 值为 3 nM。XEN907 也抑制 CYP3A4。XEN907 可用于疼痛研究。
生物活性
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
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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