Diacerein

SKU: orb1309160

Description

Diacerein is a prodrug metabolized to rhein, approved in France for osteoarthritis but limited by side effects like severe diarrhea. Current research investigates its potential for treating Type 2 Diabetes Mellitus, insulin resistance, and related complications, with studies conducted in both in vitro and in vivo models.

Research Area

Immunology & Inflammation, Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 13739-02-1
• MW: 368.29
• Purity: 98.14% (May vary between batches)
• Formula: C₁₉H₁₂O₈
• SMILES: CC(=O)OC1=CC(=CC2=C1C(=O)C1=C(OC(C)=O)C=CC=C1C2=O)C(O)=O
• Target: IL Receptor|||Interleukin
• Solubility: DMSO:6.25 mg/mL (16.97 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• In Vivo:
  Diacerein significantly reduces the activity of MMP-13 and cathepsin K in osteoclasts. It effectively blocks the effects of IL-1β on both the differentiation process of osteoclasts and the survival of mature osteoclasts. Diacerein notably inhibits IL-1β production induced by lipopolysaccharides in synovial tissues and cartilage. Dose-dependently, diacerein decreases the generation of MMP-13 induced by interleukin-1-beta (IL-1β) in osteoarthritic cartilage. At 1 μM, diacerein exhibits a notably lower inhibitory effect on cartilage synthesis compared to a medium containing only LPS. At this concentration, diacerein also reduces nitric oxide (NO) release in the synovial and cartilage culture mediums and increases IL-1ra levels in the cartilage culture medium. At 10 μM, diacerein enhances the expression of TGF-β1 and TGF-β2 in cultured bovine articular chondrocytes.
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• In Vitro:
  In ovariectomized rats, daily administration of 100 mg/kg of Diacerein significantly prevented bone loss and reduced levels of serum alkaline phosphatase, as well as diminished the excretion of hydroxyproline in urine. The same daily dose of Diacerein notably suppressed paw edema and the increase of serum mucoproteins in adjuvant-induced arthritic rats. In these rats, the combined use of 30 mg/kg Diacerein with 3 mg/kg Naproxen daily exhibited more pronounced anti-inflammatory activity than Naproxen alone. Moreover, at the lesion site on the lateral tibial plateau in Merino sheep, 25 mg/kg Diacerein reduced the thickness of the cartilage and subchondral bone.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Diacetylrhein, Diacerein, Diacerhein, inhibit, ILReceptor, IL-1β, IL Receptor, Interleukin, Interleukin Related, Inhibitor, Fisiodar

Compound Identifiers

PubChem CID

26248