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Emodin.

(Synonyms: 大黄素; Frangula emodin)

目录号: PC11531 纯度: ≥98%

天然存在的蒽醌，抗增殖,Emodin 是一种广谱抗癌剂。Emodin 抑制蛋白激酶CK2 (IC50 为 2 μM。

CAS No. :518-82-1

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中文名称

Emodin.

中文别名

大黄素;朱砂莲甲素;1,3,8-三羟基-6-甲基蒽醌;大黄素,泻素;2-甲基-4,5,7-三羟基蒽醌;6-甲基-1,3,8-三羟基蒽醌;大黄素(泻鼠李树皮);泻素;大黄素对照品;大黄素对照品标准品;大黄素标准品;大黄素植物提取物,标准品,对照品;大黄素提取物;大黄素中药对照品;何首乌提取物;决明子提取物;青蒿提取物;朱砂莲甲素植物提取物,标准品,对照品;1,3,8-三羥-6-甲蒽醌;1'3'8-三羟基-6-甲基蒽醌;大黄酸;何首乌;朱砂莲甲素.1'3'8-三羟基-6-甲基蒽醌

英文名称

Emodin

英文别名

Emodin;1,3,8-Trihydroxy-6-methylanthraquinone;6-Methyl-1,3,8-trihydroxyanthraquinone;emodin from frangula bark;2-CHLOROPYRIDINE-3-BORONIC ACID;EMODIN(P);EMODIN(P) PrintBack;EMODIN(RG);Frangula emodin;1,3,8-trihydroxy-6-methyl-9,10-anthraquinone;1,3,8-TRIHYDROXY-6-METHYL-9-10-ANTHRACENEDIONE;1,3,8-Trihydroxy-6-methylanthracene-9,10-dione;1,3,8-Tri-hydroxy-6-methyl-anthra-quinone;Alatinone;Archin;Ecdyson;Emdin;EMODIN 99;EMODINE;EMODOL;schuttgelb;1,3,8-Trihydroxy-6-methyl-9,10-anthracenedione;1,3,8-Trihydroxy-6-methylanthraquinone;6-Methyl-1,3,8-trihydroxyanthraquinone;Frangula-emodin;Frangulic acid;Rheum emodin;C.I. 75440;C.I. Natural Yellow 14;[ "1", "3", "8-Trihydroxy-6-methylanthraquinone" ];1;3-Methyl-1,6,8-trihydroxyanthraquinone;Persian Berry Lake;9,10-Anthracenedione, 1,3,8-trihydroxy-6-methyl-;4,5,7-Trihydroxy-2-methylanthraquinone;NS

Cas No.

518-82-1

分子式

C₁₅H₁₀O₅

分子量

270.24

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

详情描述

天然存在的蒽醌，抗增殖,Emodin 是一种广谱抗癌剂。Emodin 抑制蛋白激酶CK2 (IC50 为 2 μM。

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.

性状

Solid

IC50 & Target[1][2]

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.
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.
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.
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.

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

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.

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.
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.

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

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

结构分类

来源

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. [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

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

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

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

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 0.5% MC 0.5% Tween-80
Solubility: 10 mg/mL (37.00 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 3.33 mg/mL (12.32 mM); Suspened solution; Need ultrasonic

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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