Demethylasterriquinone B1
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Demethylasterriquinone B1 (DAQ B1; L-783281) is an orally active insulin receptor (insulin receptor) agonist and AKT activator. By activating AKT, Demethylasterriquinone B1 upregulates the expression and activity of eNOS to increase NO production, while downregulating the expression of the NADPH oxidase subunit p22phox to reduce oxidative stress and improve vascular endothelial dysfunction in hypertensive rats. Demethylasterriquinone B1 combind with an AKT inhibitor targets the insulin signaling pathway to activate two antiviral pathways, RNA interference and JAK/STAT, in mosquitoes, thereby reducing Zika virus infection.
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。
- 純度 : 98.10%
- CAS 番号: 78860-34-1
- 分子式: C32H30N2O4
- 分子量:506.59
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
体外実験
Demethylasterriquinone B1 (1 μM; 24 h) activates the AKT/FOXO insulin signaling pathway, increases the phosphorylation level of ERK, and upregulates the RNAi marker AGO2 in Aedes aegypti Aag2 cells[2].
Demethylasterriquinone B1 (1 μM; 24 h) significantly reduces Zika virus replication levels in Aedes aegypti Aag2 cells on day 1 and day 3 post-infection[2].
Demethylasterriquinone B1 (1 μM; 24 h) exerts antiviral activity against Zika virus in Aedes aegypti Aag2 cells, and this activity depends on functional RNAi and JAK/STAT signaling pathways[2].
Demethylasterriquinone B1 (10-50 µM) effectively reverses insulin resistance induced by PC-1 overexpression and TNF-α inflammation in HTC-IR cells, but has no effect on resistance induced by PKC activation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Combination treatment with demethylasterriquinone B1 (10 μM; p.o.; single administration) and an AKT inhibitor reduces ZIKV infection rate and viral titer in Aedes aegypti, and induces activation of the RNAi and JAK/STAT antiviral pathways, with the induction level of immune genes peaking at 7 days post-infection[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley (young male, 250-300 g; uninephrectomized + DOCA + salt water-induced hypertension)[1]
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Dosage:5 mg/kg
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Administration:p.o.; daily; 1 week
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Result:Improved the vascular endothelial dysfunction in DOCA-salt hypertensive rats.
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Animal Model:Poza Rica strain (6-9-day-old adult females)[2]
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Dosage:10 μM (in combination with 10 μM AKT inhibitor VIII)
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Administration:oral (single ZIKV-containing bloodmeal)
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Result:Simultaneously activated the RNAi and JAK/STAT two antiviral pathways in Aedes aegypti mosquitoes.
Significantly reduced the infection rate and viral load of the Zika virus in mosquitoes, especially in the salivary glands which determine the transmission ability.
化学情報
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CAS 番号 78860-34-1
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性状 Solid
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分子量 506.59
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分子式 C32H30N2O4
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Color Brown to reddish brown
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SMILES
C=CC(C)(C1=C(C(C(C(O)=C2C3=CNC4=C3C=CC=C4C/C=C(C)/C)=O)=C(O)C2=O)C5=C(C=CC=C5)N1)C
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別名
DAQ B1; L-783281; Dimethylasterriquinone
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外:
DMF : 15 mg/mL (29.61 mM; Need ultrasonic and warming)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1].
Li M, et al. Small molecule insulin receptor activators potentiate insulin action in insulin-resistant cells. Diabetes. 2001 Oct;50(10):2323-8.
[Content Brief]
[2]. Shah DI, et al. Effect of demethylasterriquinone b1 in hypertension associated vascular endothelial dysfunction. Int J Cardiol. 2007;120(3):317-324. [Content Brief]
[3]. Trammell CE, et al. Coupled small molecules target RNA interference and JAK/STAT signaling to reduce Zika virus infection in Aedes aegypti. PLoS Pathog. 2022;18(4):e1010411. Published 2022 Apr 4. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMF | 1 mM | 1.9740 mL | 9.8699 mL | 19.7398 mL | 49.3496 mL |
| 5 mM | 0.3948 mL | 1.9740 mL | 3.9480 mL | 9.8699 mL | |
| 10 mM | 0.1974 mL | 0.9870 mL | 1.9740 mL | 4.9350 mL | |
| 15 mM | 0.1316 mL | 0.6580 mL | 1.3160 mL | 3.2900 mL | |
| 20 mM | 0.0987 mL | 0.4935 mL | 0.9870 mL | 2.4675 mL | |
| 25 mM | 0.0790 mL | 0.3948 mL | 0.7896 mL | 1.9740 mL |
Keywords
- Demethylasterriquinone B1
- 78860-34-1
- DAQ B1
- L-783281
- Dimethylasterriquinone
- Demethylasterriquinone B 1
- Demethylasterriquinone B-1
- DAQ B 1
- DAQ B-1
- L783281
- L 783281
- L-783281
- Insulin Receptor
- Akt
- NO Synthase
- NADPH Oxidase
- JAK
- STAT
- FOXO
- DNA/RNA Synthesis
- ERK
- Flavivirus
- JAK/STAT signaling pathways
- p22phox
- Aedes aegypti Aag2 cells
- insulin receptor
- eNOS
- Aedes aegypti
- hypertensive rats
- Zika virus
- Sprague Dawley rats
- Inhibitor
- inhibitor
- inhibit