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VU041
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。
VU041图片
CAS NO:332943-64-3
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
VU041 是第一个亚微摩尔亲和力 Anopheles (An.) gambiae 和 Aedes (Ae.) aegypti Kir1 通道的抑制剂,IC50 值分别为 2.5 μM 和 1.7 μM。VU041 明显抑制哺乳动物 Kir2.1 通道 (IC50 为12.7 μM),对哺乳动物 Kir1.1,Kir4.1,Kir6.2/SUR1 和 Kir7.1 的抑制作用较小。VU041 也可导致 Malpighian 小管功能受损。
Cas No.332943-64-3
分子式C19H20F3N3O
分子量363.38
溶解度DMSO : 20 mg/mL (55.04 mM; ultrasonic and warming and heat to 60°C)
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

VU041 is a first submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegypti inward rectifier potassium 1 (Kir1) channels with IC50 values of 2.5 μM and 1.7 μM, respectively. VU041 inhibits appreciably is mammalian Kir2.1 (IC50 of 12.7 μM), and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. VU041 also induces impaired Malpighian tubule function[1].

VU041 is only moderately metabolized by cytochrome P450 enzymes and does not appear to be metabolized by esterases. VU041 is the first small-molecule inhibitor of mosquito Kir1 channels that exhibits topical toxicity in both insecticide-susceptible and -resistant lines of mosquitoes[1].

Topical VU041 application to adult female mosquitoes of both species inhibits their fecundity. Importantly, VU041 is selective for mosquito Kir channels over mammalian Kir channel orthologs and non-lethal to adult honey bees (Apis mellifera). The in vivo experiments of blood meal processing and diuretic capacity suggest that one mechanism of action of VU041 is the disruption of excretory functions mediated by Malpighian tubules[1].

[1]. Swale DR, et al. An insecticide resistance-breaking mosquitocide targeting inward rectifier potassium channels in vectors of Zika virus and malaria. Sci Rep. 2016 Nov 16;6:36954.