1. Immunology/Inflammation Neuronal Signaling Membrane Transporter/Ion Channel
  2. Interleukin Related Calcium Channel
  3. Diacerein

Diacerein  (Synonyms: 双醋瑞因; Diacerhein; Diacetylrhein)

目录号: HY-N0283 纯度: 98.78%
COA 产品使用指南

Diacerein (Diacerhein) 是一种具有口服活性的蒽醌,可减少 IL-1 转换酶的产生,然后通过相关下游信号传导抑制 IL-1β 的激活。Diacerein 是一种抗炎和抗风湿剂。Diacerein 可以缓解哮喘小鼠的支气管痉挛并控制气道炎症。Diacerein 具有用于骨关节炎研究的潜力。

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Diacerein Chemical Structure

Diacerein Chemical Structure

CAS No. : 13739-02-1

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥614
In-stock
50 mg ¥558
In-stock
100 mg ¥1004
In-stock
200 mg   询价  
500 mg   询价  

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Customer Review

Other Forms of Diacerein:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Diacerein (Diacerhein), an orally active anthraquinone, reduces production of IL-1 converting enzyme then inhibits the activation of IL-1β by related downstream signaling. Diacerein is an anti-inflammatory and anti-rheumatic drug. Diacerein can relieve bronchospasm and control airway inflammation in asthmatic mice. Diacerein has the potential for slow acting drug in osteoarthritis (SYSADOA) research[1][2][3].

IC50 & Target[1]

IL-1β

 

L-type calcium channel

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
RAW264.7 IC50
106.9 μM
Compound: Diacerein
Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-6 production incubated for 48 hrs by ELISA analysis
Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-6 production incubated for 48 hrs by ELISA analysis
[PMID: 34491054]
RAW264.7 CC50
108.2 μM
Compound: Diacerein
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
[PMID: 34491054]
RAW264.7 IC50
126.77 μM
Compound: Diacerein
Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in TNF-alpha production incubated for 48 hrs by ELISA analysis
Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in TNF-alpha production incubated for 48 hrs by ELISA analysis
[PMID: 34491054]
RAW264.7 IC50
65.41 μM
Compound: Diacerein
Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-1beta production incubated for 48 hrs by ELISA analysis
Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as reduction in IL-1beta production incubated for 48 hrs by ELISA analysis
[PMID: 34491054]
体外研究
(In Vitro)

Diacerein (Diacerhein;30-300 μM;24、48 小时) 可降低软骨肉瘤细胞的增殖和活力[1]
Diacerein (30-300 μM;48 小时) 会导致 SW-1353 细胞周期 G2/M 停滞[1]
Diacerein (30-300 μM;48 小时) 会降低 SW-1353 细胞周期蛋白 B1、CDK1 和 CDK2 水平[1]
Diacerein 可通过电压依赖性 L 型 Ca2+ 通道、非选择性阳离子通道、大电导 Ca2+ 激活的 K+ 通道和 Na+/Ca2+ 介导的细胞内和细胞外钙动员来松弛激动剂预收缩的小鼠气道平滑肌交换体[2].

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

Cell Viability Assay[1]

Cell Line: Cal-78 and SW-1353 cells
Concentration: 30, 100, and 300 μM
Incubation Time: 24, 48 h
Result: Inhibited cell growth in a concentration dependent manner in both cell lines.

Cell Cycle Analysis[1]

Cell Line: Cal-78 and SW-1353 cells
Concentration: 30, 100, and 300 μM
Incubation Time: 48 h
Result: Caused a pronounced decrease in the number of cells in the G1 phase, accompanied by a significant increase of the number of S and G2/M phase cells, indicating a G2/M arrest in SW-1353 cells.

Western Blot Analysis[1]

Cell Line: Cal-78 and SW-1353 cells
Concentration: 30, 100, and 300 μM
Incubation Time: 24 h
Result: Induced a small, but not significant change, for the expression of CDK1, whereas the cyclin B1 and CDK2 levels were significantly down-regulated in the case of Cal-78 cells.
体内研究
(In Vivo)

Diacerein (Diacerhein;50、100、200 mg/kg;灌胃;每天;一周) 可有效降低卵白蛋白 (OVA;3 mg/ml;200 μl;IP;用 25 mg/ml Al(OH)3,第 1 天、第 8 天) 诱导的哮喘小鼠的气道高血压并改善气道重塑[2]
Diacerein (2、20、60 mg/kg;每日;口服;2 周龄转基因小鼠;持续 5 周) 在 Tg197 转基因关节炎 (RA)小鼠模型中不仅显着减少软骨破坏,也显着减少滑膜炎和骨侵蚀程度[3]

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

Animal Model: Male BALB/c mice at 6-8 weeks of age[2]
Dosage: 50, 100, 200 mg/kg
Administration: Gavaged; daily; a week
Result: Reduced systematic inflammation and mucus secretion in vivo.
Exhibited anti-inflammatory property to significantly reduce inflammation and repair damaged airway.
Clinical Trial
分子量

368.29

Formula

C19H12O8

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

双醋瑞因;达赛瑞英;二乙酰大黄酸

结构分类
初始来源
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 1 year
-20°C 6 months
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 12.5 mg/mL (33.94 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7153 mL 13.5763 mL 27.1525 mL
5 mM 0.5431 mL 2.7153 mL 5.4305 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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: 1% CMC/saline water

    Solubility: 5 mg/mL (13.58 mM); 悬浊液; Need ultrasonic and warming and heat to 40°C

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.78%

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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6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
DMSO 1 mM 2.7153 mL 13.5763 mL 27.1525 mL 67.8813 mL
5 mM 0.5431 mL 2.7153 mL 5.4305 mL 13.5763 mL
10 mM 0.2715 mL 1.3576 mL 2.7153 mL 6.7881 mL
15 mM 0.1810 mL 0.9051 mL 1.8102 mL 4.5254 mL
20 mM 0.1358 mL 0.6788 mL 1.3576 mL 3.3941 mL
25 mM 0.1086 mL 0.5431 mL 1.0861 mL 2.7153 mL
30 mM 0.0905 mL 0.4525 mL 0.9051 mL 2.2627 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    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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Diacerein
目录号:
HY-N0283
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