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

Diacerein  (Synonyms: Diacerhein; Diacetylrhein)

Cat. No.: HY-N0283 Purity: 98.78%
COA Handling Instructions

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

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Solid
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100 mg USD 143 In-stock
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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Diacerein

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  • Customer Review

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

 

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.

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)

H2O : ≥ mg/mL

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2715 mL 1.3576 mL 2.7153 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  1% (w/v) carboxymethylcellulose (CMC)

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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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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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HY-N0283
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