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大黄素 促销  ≥98%(HPLC),分析标准品

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包装规格：20mg in glass bottle
产品简介：一种蒽醌衍生物，是一种抗 COVID-19 化合物。Emodin 阻断 SARS 病毒刺突蛋白和血管紧张素转化酶 2 (ACE2) 的相互作用。Emodin 抑制酪蛋白激酶 2 (CK2)。 具有抗炎和抗癌作用。Emodin 还是一种有效的选择性 11β-HSD1 抑制剂，对人和小鼠 11β-HSD1 的 IC50 分别为 186 和 86 nM。Emodin 可改善饮食诱导的肥胖小鼠的代谢紊乱。
溶解性：溶于10mg/mL氢氧化铵溶液
储备液保存：-80°C, 1 year -20°C, 6 months
体内实验：1、请依序添加每种溶剂： 0.5% CMC-Na/saline water Solubility: 3.33 mg/mL (12.32 mM); Suspened solution; 超声助溶 2、请依序添加每种溶剂： 0.5% Methyl cellulose/0.5% Tween-80 in Saline water Solubility: 10 mg/mL (37.00 mM); 悬浊液; 超声助溶
靶点：SARS-CoV CK2α Wild-type Q1.4 μM (IC50, at ATP concentration is 10 μM) CK2α Wild-type mouse 11β-HSD1 5.9 μM (IC50, at ATP concentration is 50 μM) 6 nM (IC50) human 11β-HSD1 186 nM (IC50)
体外研究：Emodin (10-400 μM) 以剂量依赖性方式阻断 S 蛋白与 ACE2 的结合，IC50 值为 200 μM。 Emodin (5-50 μM) 以剂量依赖的方式抑制 S 蛋白假型逆转录病毒的感染性。Emodin 阻断 SARS-CoV S 蛋白与 Vero E6 细胞的结合。 Emodin 抑制酪蛋白激酶 2 (CK2)，IC50 为 5.9 CK2α 野生型、Ile174Ala 突变体和 His160Ala 突变体在 ATP 浓度下分别为 50 μM、30.0 和 7.1 μM。CK2α 野生型的 IC50 分别为 1.40 和 38.00 μM，Val66Ala 突变体在 ATP 浓度下为 10 μM。 Emodin 表现出低抑制性对小鼠和人类 2 型 11β-羟基类固醇脱氢酶的活性，IC50 高于 1 mM，表明 Emodin 对人类和小鼠 11β-的选择性超过 5000 倍HSD1 酶超过 2 型同工酶。
体内研究：Emodin (单次口服100或200 mg/kg) 抑制正常C57BL/6J雄性小鼠11β-HSD1活性。 Emodin (100 mg/kg；口服；bid) 改善饮食诱导的肥胖 (DIO) 小鼠的胰岛素敏感性和脂质代谢，降低血糖和肝脏 PEPCK 以及葡萄糖-6-磷酸酶 mRNA。
细胞实验：Cell Viability Assay Cell Line: Vero E6 cells transfected with the plasmid encoding ACE2 Concentration: 0, 5, 25, 50 μM Incubation Time: 24 hours Result: Vero cells treated with 50 μM remained 82.4±3.8% viability, the anti-SARS-CoV activity was not due to toxicity.
动物实验：Animal Model: C57BL/6J male mice Dosage: 100 or 200 mg/kg Administration: Acute administered p.o. ; Two hours later, the mice were killed by cervical dislocation, Result: Significantly inhibited liver 11β-HSD1 enzymatic activity by 17.6 and 31.3% and mesenteric fat 11β-HSD1 enzymatic activity by 21.5 and 46.7% at 100 or 200 mg/kg, respectively. Animal Model: DIO mice (C57BL/6J male mice were fed a formulated research diet) Dosage: 100 mg/kg Administration: Oral gavage; twice per day; for 35 days Result: Reduced fasting glucose concentrations to 77.2% of the vehicle control mice after 7 days of treatment, and these remained significantly lower throughout the treatment period. Exhibited a significant reduction in blood glucose levels at all time-points following oral glucose challenge after 24 days of treatment. Evoked a significantly greater reduction in blood glucose values 40 and 90 min after insulin injection after 28 days of treatment. The serum insulin level was also significantly reduced, to 66.2% of control mice, after 35 days of treatment. Improved the lipid profiles. The serum triglyceride and total cholesterol levels were significantly reduced by 19.3 and 12.5% after 35 days of treatment, respectively. Caused a 22.7% reduction of non-esterified free fatty acid (NEFA) level. Lowered body weight and appetite from day 18 of the treatment; their body weights were reduced by 13.9% at the end of treatment.
保存条件：2-8℃
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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