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 to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing.
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
in solvent
Synonyms N/A

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03472287 Recruiting Epidermolysis Bullosa Castle Creek Pharmaceuticals LLC May 10 2018 Phase 1
NCT03472547 Completed Skin Pigment Castle Creek Pharmaceuticals LLC January 15 2018 Phase 1
NCT03472534 Completed Healthy Castle Creek Pharmaceuticals LLC January 9 2018 Phase 1
NCT03404479 Recruiting Knee Osteoarthritis Whan-Seok Choi|Korea University Guro Hospital|Seoul St. Mary''s Hospital January 25 2018 Phase 4
NCT03473197 Completed Healthy Castle Creek Pharmaceuticals LLC January 8 2018 Phase 1
NCT03389308 Enrolling by invitation Epidermolysis Bullosa Simplex Castle Creek Pharmaceuticals LLC December 1 2017 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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