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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1689545-27-4
- 分子式: C17H16N4O
- 分子量:292.34
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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.
化学情報
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CAS 番号 1689545-27-4
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分子量 292.34
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)