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.
Product information
CAS Number: 332943-64-3
Molecular Weight: 363.38
Formula: C19H20F3N3O
Chemical Name: 1-(1,2,3,4-tetrahydroquinolin-1-yl)-2-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]ethan-1-one
Smiles: O=C(CN1N=C(C2CCCCC1=2)C(F)(F)F)N1CCCC2=CC=CC=C12
InChiKey: DLAGRCZUELSZFG-UHFFFAOYSA-N
InChi: InChI=1S/C19H20F3N3O/c20-19(21,22)18-14-8-2-4-10-16(14)25(23-18)12-17(26)24-11-5-7-13-6-1-3-9-15(13)24/h1,3,6,9H,2,4-5,7-8,10-12H2
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 20 mg/mL (55.04 mM; ultrasonic and warming and heat to 60°C).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
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