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  3. Demethylasterriquinone B1

Demethylasterriquinone B1  (Synonyms: DAQ B1; L-783281; Dimethylasterriquinone)

目录号: HY-107586
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纯度: 98.10%
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Demethylasterriquinone B1 (DAQ B1; L-783281) 是一种具有口服活性的胰岛素受体 (insulin receptor) 激动剂和 AKT 激活Demethylasterriquinone B1 通过激活 Akt,进而上调 eNOS 表达和活性、增加 NO 生成,同时下调 NADPH 氧化酶亚基 p22phox 表达、减少氧化应激,高血压大鼠的血管内皮功能障碍。Demethylasterriquinone B1 和 AKT 抑制剂联合用药,通过靶向胰岛素信号通路,激活蚊子的 RNA 干扰和 JAK/STAT 两条抗病毒通路,从而减少寨卡病毒感染。

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Demethylasterriquinone B1

Demethylasterriquinone B1 Chemical Structure

CAS No. : 78860-34-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2][3].

体外研究
(In Vitro)

Demethylasterriquinone B1 (1 μM; 24 h) 激活 AKT/FOXO 胰岛素信号通路,提高 ERK 磷酸化水平,并在埃及伊蚊 Aag2 细胞中上调 RNAi 标志物 AGO2[2]
Demethylasterriquinone B1 (1 μM; 24 h) 可显著降低埃及伊蚊 Aag2 细胞在感染后第 1 天和第 3 天的寨卡病毒复制水平[2]
Demethylasterriquinone B1 (1 μM; 24 h) 在埃及伊蚊 Aag2 细胞中对寨卡病毒发挥抗病毒作用,该作用依赖于功能性 RNAi 和 JAK/STAT 信号通路[2]
Demethylasterriquinone B1 (10-50 µM) 在 HTC-IR 细胞中能有效逆转由 PC-1 过表达和 TNF-α 炎症引起的胰岛素抵抗,但对 PKC 激活引起的抵抗无效[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Demethylasterriquinone B1 (5 mg/kg; 口服; 每日一次共一周) 可通过恢复 eNOS 活性、减轻氧化应激并降低雄性 Sprague Dawley 大鼠的平均动脉血压,改善高血压相关的血管内皮功能障碍,且其作用依赖于 eNOS 活性[1]
Demethylasterriquinone B1 (10 μM; 口服; 单次给药) 和 AKT 抑制剂连用后可降低埃及伊蚊(Aedes aegypti) 中的 ZIKV 感染率与病毒滴度,并诱导 RNAi 和 JAK/STAT 抗病毒通路激活,感染后 7 天免疫基因诱导水平达到峰值[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague Dawley (young male, 250-300 g; uninephrectomized + DOCA + salt water-induced hypertension)[1]
Dosage: 5 mg/kg
Administration: p.o.; daily; 1 week
Result: Improved the vascular endothelial dysfunction in DOCA-salt hypertensive rats.
Animal Model: Poza Rica strain (6-9-day-old adult females)[2]
Dosage: 10 μM (in combination with 10 μM AKT inhibitor VIII)
Administration: oral (single ZIKV-containing bloodmeal)
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.
分子量

506.59

Formula

C32H30N2O4

CAS 号
性状

固体

颜色

Brown to reddish brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMF 中的溶解度 : 15 mg/mL (29.61 mM; 超声加热助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9740 mL 9.8699 mL 19.7398 mL
5 mM 0.3948 mL 1.9740 mL 3.9480 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

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  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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体积 (start)

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体积 (final)

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动物溶解方案计算器
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给药剂量

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动物的平均体重

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工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.10%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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目录号:
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