VU041|332943-64-3|-陌孚医药/Medlife

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VU041

目录号: PL10023 纯度: ≥99%

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

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中文名称	VU041
英文名称	VU041
英文别名	1-(3,4-Dihydro-2H-quinolin-1-yl)-2-(3-trifluoromethyl-4,5,6,7-tetrahydro-in dazol-1-yl)-ethanone;VU041
Cas No.	332943-64-3
分子式	C₁₉H₂₀N₃OF₃
分子量	363.38
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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。
生物活性	VU041 is a first submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegypti inward rectifier potassium 1 (Kir1) channels with IC 50 values of 2.5?μM and 1.7?μM, respectively. VU041 inhibits appreciably is mammalian Kir2.1 (IC 50 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.
性状	Solid
IC50 & Target[1][2]	IC50: 2.5?μM (Anopheles (An.) gambiae Kir1 channels), 1.7?μM (Aedes (Ae.) aegypti Kir1 channels) and 12.7?μM (Mammalian Kir2.1)
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. 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]. 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.

溶解度数据	In Vitro: DMSO : 20 mg/mL (55.04 mM; ultrasonic and warming and heat to 60°C)配制储备液

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