产品
编 号：F376888
分子式：C15H10O5
分子量：270.24
分子式：C15H10O5
分子量：270.24
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
50mg
160
In-stock
100mg
256
In-stock
200mg
410
In-stock
结构图
CAS No: 518-82-1
产品详情
生物活性：
Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
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。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.
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 (11β-HSD2) 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。
Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
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。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.
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 (11β-HSD2) 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。
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