标签归档：frangula

Emodin(Synonyms: 大黄素; Frangula emodin)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Emodin (Synonyms: 大黄素; Frangula emodin) 纯度: 99.39%

Emodin (Frangula emodin) 是一种蒽醌衍生物，是一种抗 SARS-CoV 化合物。Emodin 阻断 SARS 冠状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。

Emodin(Synonyms: 大黄素; Frangula emodin)

Emodin Chemical Structure

CAS No. : 518-82-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥385 In-stock
50 mg ￥350 In-stock
100 mg ￥560 In-stock
200 mg ￥1000 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Emodin 相关产品

•相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Natural Product Library
  • Anti-Cancer Compound Library
  • Antiviral Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Diabetes Related Compound Library
  • Phenols Library
  • Traditional Chinese Medicine Monomer Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Obesity Compound Library
  • Food-Sourced Compound Library
  • Rare Diseases Drug Library

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[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. 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[3].

IC50 & Target[1][2][3]

SARS-CoV

 

CK2α Wild-type

1.4 μM (IC50, at ATP concentration is 10 μM)

CK2α Wild-type

5.9 μM (IC50, at ATP concentration is 50 μM)

mouse 11β-HSD1

86 nM (IC50)

human 11β-HSD1

186 nM (IC50)

体外研究
(In Vitro)

Emodin (10-400 μM) blocks the binding of S protein to ACE2 in a dose-dependent manner with the IC50 value of 200 μM[1].
Emodin (5-50 μM) inhibits the S protein-pseudotyped retrovirus infectivity in a dose-dependent manner. Emodin blocks the SARS-CoV S protein binding to Vero E6 cells[1].
Emodin inhibits casein kinase-2 (CK2) with IC50s of 5.9, 30.0, and 7.1 μM for CK2α Wild-type, Ile174Ala mutant, and His160Ala mutant at ATP concentration is 50 μM, respectively. The IC50s are 1.40 and 38.00 μM for CK2α Wild-type, and Val66Ala mutant at ATP concentration is 10 μM[2].
Emodin exhibits low inhibitory activity against mouse and human 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), with an IC50 higher than 1 mM, indicating that Emodin is more than 5000-fold selective for the human and mouse 11β-HSD1 enzymes over the type 2 isoenzyme[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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.

体内研究
(In Vivo)

Emodin (single oral administration of 100 or 200 mg/kg) inhibits 11β-HSD1 activity in normal C57BL/6J male mice[3].
Emodin (100 mg/kg; oral administration; b.i.d.) improves insulin sensitivity and lipid metabolism, and lowers blood glucose and hepatic PEPCK, and glucose-6-phosphatase mRNA in diet-induced obese (DIO) mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J male mice[3]
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)[3]
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.

Clinical Trial

分子量

270.24

Formula

C15H10O5
CAS 号

518-82-1
中文名称

大黄素
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

Acetone : 10.87 mg/mL (40.22 mM; Need ultrasonic)

DMSO : 5.41 mg/mL (20.02 mM; Need ultrasonic)

Ethanol : < 1 mg/mL (ultrasonic) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7004 mL 18.5021 mL 37.0041 mL
5 mM 0.7401 mL 3.7004 mL 7.4008 mL
10 mM 0.3700 mL 1.8502 mL 3.7004 mL

*

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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 0.5% MC  0.5% Tween-80

    Solubility: 10 mg/mL (37.00 mM); Suspended solution; Need ultrasonic

  • 2.

    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; Need ultrasonic

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Tin-Yun Ho, et al. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 interaction. Antiviral Res. 2007 May;74(2):92-101.

    [2]. Stefania Sarno, et al. Toward the rational design of protein kinase casein kinase-2 inhibitors. Pharmacol Ther. Feb-Mar 2002;93(2-3):159-68.

    [3]. Ying Feng, et al. Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice. Br J Pharmacol. 2010 Sep;161(1):113-26.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Emodin-d4(Synonyms: Frangula emodin-d4)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Emodin-d4 (Synonyms: Frangula emodin-d4)

Emodin-d4 (Frangula emodin-d4) 是 Emodin 的氘代物。Emodin (Frangula emodin) 是一种蒽醌衍生物，是一种抗 SARS-CoV 化合物。Emodin 阻断 SARS 冠状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。

Emodin-d4(Synonyms: Frangula emodin-d4)

Emodin-d4 Chemical Structure

CAS No. : 132796-52-2

规格 是否有货
1 mg Check price and availability
10 mg Check price and availability

* Please select Quantity before adding items.

生物活性

Emodin-d4 (Frangula emodin-d4) is the deuterium labeled Emodin. 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[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. 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[3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

274.26

Formula

C15H6D4O5
CAS 号

132796-52-2
中文名称

大黄素 d4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Tin-Yun Ho, et al. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 interaction. Antiviral Res. 2007 May;74(2):92-101.

    [3]. Stefania Sarno, et al. Toward the rational design of protein kinase casein kinase-2 inhibitors. Pharmacol Ther. Feb-Mar 2002;93(2-3):159-68.

    [4]. Ying Feng, et al. Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice. Br J Pharmacol. 2010 Sep;161(1):113-26.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务