1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. VU041

VU041 

Cat. No.: HY-118607 Purity: 99.64%
Handling Instructions

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.

For research use only. We do not sell to patients.

VU041 Chemical Structure

VU041 Chemical Structure

CAS No. : 332943-64-3

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10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
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10 mg USD 140 In-stock
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25 mg USD 300 In-stock
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50 mg USD 500 In-stock
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100 mg USD 850 In-stock
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Description

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].

IC50 & Target

IC50: 2.5 μM (Anopheles (An.) gambiae Kir1 channels), 1.7 μM (Aedes (Ae.) aegypti Kir1 channels) and 12.7 μM (Mammalian Kir2.1)[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

363.38

Formula

C₁₉H₂₀F₃N₃O

CAS No.

332943-64-3

SMILES

FC(C1=NN(CC(N2CCCC3=C2C=CC=C3)=O)C4=C1CCCC4)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (55.04 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7519 mL 13.7597 mL 27.5194 mL
5 mM 0.5504 mL 2.7519 mL 5.5039 mL
10 mM 0.2752 mL 1.3760 mL 2.7519 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2 mg/mL (5.50 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2 mg/mL (5.50 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (5.50 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

VU041VU 041VU-041Potassium ChannelKcsAKir1insecticidesresistancemosquitoesmammalianKir2.1CYP450MalpighiantubulesmosquitocidesInhibitorinhibitorinhibit

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VU041
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