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

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

目錄號: HY-N0283 純度: 98.78%
COA 產(chǎn)品使用指南

Diacerein (Diacerhein) 是一種具有口服活性的蒽醌，可減少 IL-1 轉(zhuǎn)換酶的產(chǎn)生，然后通過相關(guān)下游信號傳導抑制 IL-1β 的激活。Diacerein 是一種抗炎和抗風濕劑。Diacerein 可以緩解哮喘小鼠的支氣管痙攣并控制氣道炎癥。Diacerein 具有用于骨關(guān)節(jié)炎研究的潛力。

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Diacerein Chemical Structure

Diacerein Chemical Structure

CAS No. : 13739-02-1

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2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥614
In-stock
50 mg ￥558
In-stock
100 mg ￥1004
In-stock
200 mg   詢價  
500 mg   詢價  

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Customer Review

Other Forms of Diacerein:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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

 

細胞效力
(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]
體外研究
(In Vitro)

Diacerein (Diacerhein；30-300 μM；24、48 小時) 可降低軟骨肉瘤細胞的增殖和活力[1]。
Diacerein (30-300 μM；48 小時) 會導致 SW-1353 細胞周期 G2/M 停滯[1]。
Diacerein (30-300 μM；48 小時) 會降低 SW-1353 細胞周期蛋白 B1、CDK1 和 CDK2 水平[1]。
Diacerein 可通過電壓依賴性 L 型 Ca2+ 通道、非選擇性陽離子通道、大電導 Ca2+ 激活的 K+ 通道和 Na+/Ca2+ 介導的細胞內(nèi)和細胞外鈣動員來松弛激動劑預(yù)收縮的小鼠氣道平滑肌交換體[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.
體內(nèi)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) 誘導的哮喘小鼠的氣道高血壓并改善氣道重塑[2]。
Diacerein (2、20、60 mg/kg；每日；口服；2 周齡轉(zhuǎn)基因小鼠；持續(xù) 5 周) 在 Tg197 轉(zhuǎn)基因關(guān)節(jié)炎 (RA)小鼠模型中不僅顯著減少軟骨破壞，也顯著減少滑膜炎和骨侵蝕程度[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 號
性狀

固體

顏色

Light yellow to yellow

中文名稱

雙醋瑞因；達賽瑞英；二乙酰大黃酸
結(jié)構(gòu)分類
初始來源
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 12.5 mg/mL (33.94 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗：

以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑： 1% CMC/saline water

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

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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
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