Diacerein

Catalog No.S4267

Diacerein Chemical Structure

Molecular Weight(MW): 368.29

Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.

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1 Customer Review

  • f, Intra-TG injection of IL-1β inhibitor, Diacerein 10 days after pIONL alleviated pIONL-induced mechanical allodynia from 1 to 6 h. *P < 0.05, ***P < 0.001. Two-way repeated measures ANOVA followed by Bonferroni test.

    J Neuroinflammation, 2016, 13(1):183.. Diacerein purchased from Selleck.

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Biological Activity

Description Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.
In vitro

Diacerein significantly inhibits LPS-induced IL-1beta production by synovial tissue and cartilage. Diacerein (1 μM) has a significantly less inhibitory effect on cartilage synthesis than culture media containing LPS only. Diacerein (1 μM) decreases NO release in synovial tissue and cartilage media and increases IL-1ra levels in cartilage culture media. [1] Diacerein (10 μM) enhances the expression of TGF-beta1 and TGF-beta2 in cultured bovine articular chondrocytes. [2] Diacerein reduces, in a dose-dependent manner, the interleukin-1-beta (IL-1beta)-induced MMP-13 production in osteoarthritic subchondral bone. Diacerein significantly reduces the activity of MMP-13 and cathepsin K in osteoclasts. Diacerein effectively blocks the IL-1beta effect on the osteoclast differentiation process and the survival of mature osteoclasts. [3]

In vivo Diacerein (100 mg/kg/day) significantly suppresses the paw edema and the increase in serum mucoprotein in the adjuvant-induced arthritic rats. Diacerein (30 mg/kg/day) combined with Naproxen (3 mg/kg/day) results in significantly greater anti-inflammatory activity than with naproxen alone in the adjuvant-induced arthritic rats. Diacerein (100 mg/kg/day) also significantly prevents bone loss and reduces the serum alkaline phosphatase and decreases the excretion of urinary hydroxyproline in the ovariectomized rats. [4] Diacerein (25 mg/kg) decreases the thickness of cartilage and subchondral bone in the lesion (middle) zone of the lateral tibial plateau in Merino wethers. [5]

Protocol

Solubility (25°C)

In vitro DMSO 48 mg/mL (130.33 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
1% CMC Na
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 368.29
Formula

C19H12O8

CAS No. 13739-02-1
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02688400 Recruiting Osteoarthritis|Osteoarthritis, Knee TRB Chemedica International SA|ArthroLab Inc. May 2016 Phase 3
NCT02242149 Recruiting Type 2 Diabetes.|Non-alcoholic Fatty Liver Disease Universidade Federal do Rio de Janeiro|Rio de Janeiro State Research Supporting Foundation (FAPERJ) September 2014 Phase 3
NCT01906801 Completed Osteoarthritis|Glucosamine|Diacerein Ramathibodi Hospital July 2013 Phase 4
NCT02177643 Recruiting Diabetes-Related Complications|Diabetes Mellitus, Type 2|Insulin Resistance University of Campinas, Brazil|Conselho Nacional de Desenvolvimento Científico e Tecnológico|ANS Pharma January 2013 Phase 2
NCT02060552 Completed Primary Gout Tongji Hospital January 2013 Phase 4
NCT01264211 Completed Rheumatoid Arthritis TRB Chemedica October 2010 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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