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

Diacerein  (Synonyms: Diacerhein; Diacetylrhein)

Cat. No.: HY-N0283 Purity: 98.78%
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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.

For research use only. We do not sell to patients.

Diacerein Chemical Structure

Diacerein Chemical Structure

CAS No. : 13739-02-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 87 In-stock
Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Solid
50 mg USD 79 In-stock
100 mg USD 143 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

Other Forms of Diacerein:

Diacerein Related Antibodies

Top Publications Citing Use of Products

View All Interleukin Related Isoform Specific Products:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • Biological Activity

  • Purity & Documentation

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Description

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

 

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]
In Vitro

Diacerein (Diacerhein; 30-300 μM; 24, 48 h) reduces cell proliferation and viability of chondrosarcoma cells[1].
Diacerine (30-300 μM; 48 h) causes a SW-1353 cell cycle G2/M arrest[1].
Diacerein (30-300 μM; 48 h) decreases cyclin B1, CDK1, and CDK2 levels in SW-1353 cell[1].
Diacerein can relax the agonist-precontracted mouse airway smooth muscle via intracellular and extracellular calcium mobilization which is mediated by switched voltage-dependent L-type Ca2+ channels, non-selective cation channels, large-conductance Ca2+-activated K+ channel, and Na+/Ca2+ exchangers[2].

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

Diacerein Related Antibodies

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.
In Vivo

Diacerein (Diacerhein; 50, 100, 200 mg/kg; Gavaged; daily; a week) can effectively reduce airway hypertension and improve airway remodeling in asthmatic mice with Ovalbumin (OVA; 3 mg/ml; 200 μl; IP; dissolved with 25 mg/ml Al(OH)3 at day 1, day 8)[2].
Diacerein (2, 20, 60 mg/kg; daily; oral; at 2 weeks of age transgenic mice; for 5 weeks) reveales a significant reduction not only in cartilage destruction but also in the extent of synovitis and bone erosion in the Tg197 transgenic murine model of RA[3].

MedChemExpress (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
Molecular Weight

368.29

Formula

C19H12O8
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C(C=C1C2=O)=CC(OC(C)=O)=C1C(C3=C2C=CC=C3OC(C)=O)=O)O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (33.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  1% CMC/saline water

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 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
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Diacerein Related Classifications

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.

Keywords:

Diacerein13739-02-1Diacerhein DiacetylrheinInterleukin RelatedCalcium ChannelILCa2+ channelsCa channelsanthraquinoneIL-1 converting enzymeIL-1βanti-inflammatoryanti-rheumaticbronchospasmairway inflammationasthmaticosteoarthritisSYSADOAInhibitorinhibitorinhibit

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