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.
For research use only. We do not sell to patients.
- CAS No.: 1689545-27-4
- Formula: C17H16N4O
- Molecular Weight:292.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
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. Further protocols information, click here.
In Vivo
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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Molecular Weight 292.34
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Indazapyroxamet Related Classifications
HY-186215 Related Classifications
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