化学性质:
规格 | 10mM*1 mL in DMSO 5 mg 10 mg 25 mg 50 mg 100 mg |
CAS | 332943-64-3 |
别名 | N/A |
化学名 | N/A |
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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
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.
特别提醒:
1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。
2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。
标签:VU041
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