您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > XEN907
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
XEN907
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
XEN907图片
CAS NO:912656-34-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议

产品介绍
XEN907是一种新型的螺羟吲哚类NaV1.7阻断剂,抑制hNaV1.7,IC50为3nM。
Cas No.912656-34-9
Canonical SMILESO=C(C12COC3=C1C=C(OCO4)C4=C3)N(CCCCC)C5=C2C=CC=C5
分子式C21H21NO4
分子量351.4
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

XEN907 is a novel spirooxindole NaV1.7 blocker, inhibits hNaV1.7 with IC50 of 3 nM.IC50 value: 3 nMTarget: NaV1.7in vitro: XEN907 shows a further 10-fold increase in potency, represents a promising structure for further optimization efforts. XEN907 shows no significant activity at 10 μM against a broad panel of 63 receptors and transporters. Determination of the ADME properties of XEN907 reveals that XEN907 is not cytotoxic and has favourable hepatocyte metabolic stability for both human and dog, although inhibition of CYP3A4 is observed in a recombinant human enzyme assay.[1]in vivo: Pharmacokinetic analysis in rats of XEN907 demonstrates that, consistent with the compound's ADME parameters, the compound is modestly bioavailable. Following an initial rapid absorption phase (oral Tmax = 20 min), XEN907 is extensively distributed (Vss 600-fold higher than the plasma volume in rats) and rapidly cleared. [1]

[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.