Indazapyroxamet
Indazapyroxamet is an orally active insect TRPV channel (Nan/Iav subunit) modulator and insecticide. Indazapyroxamet antagonizes nicotinamide-induced calcium influx, inhibits insect motor function, and impairs negative geotaxis in wild-type Drosophila melanogaster via functional TRPV channels.
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- CAS No.: 1689545-27-4
- Formule: C17H16N4O
- Masse moléculaire:292.34
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Indazapyroxamet (10 min) acts as a low-efficacy partial agonist (EC50=13.1 nM) and potent antagonist (IC50=8.1 nM) of the brown planthopper TRPV channel expressed in Drosophila S2 cells[1].
Indazapyroxamet binds to the brown planthopper TRPV channel in a pocket overlapping that of known agonists, forming a π-stacking interaction with NlIavW322 but lacking critical interactions with NlNanY178, which explains its partial agonist and antagonistic activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:w1118 (wild-type, adult males, 2-4 days post eclosion); nan36ᵃ (adult males, 2-4 days post eclosion); iav1 (adult males, 2-4 days post eclosion); iav3621 (adult males, 2-4 days post eclosion)[1]
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Dosage:50 μM; 100 μM; 200 μM; 400 μM
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Administration:p.o.; single 3-hour feeding
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Result:Reduced climbing index to ~0.65 in wild-type w1118 flies at 50 μM.
Reduced climbing index to ~0.52 in wild-type w1118 flies at 100 μM.
Reduced climbing index to ~0.32 in wild-type w1118 flies at 200 μM.
Reduced climbing index to ~0.18 in wild-type w1118 flies at 400 μM.
Left climbing index unchanged in nan36ᵃ, iav1, and iav3621 TRPV loss-of-function mutants across all tested concentrations.
Chemical Information
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CAS No. 1689545-27-4
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Masse moléculaire 292.34
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Formule C17H16N4O
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SMILES
O=C(C1=CC=CC2=NN(C3=CC=CN=C3)C=C21)NC4(CC4)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Indazapyroxamet Related Classifications
HY-186215 Related Classifications
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