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Diacerein Interleukins inhibitor

Cat.No.S4267

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

Batch: Purity: 99.25%
99.25

Solubility

In vitro
Batch:

DMSO : 18 mg/mL (48.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 368.29 Formula

C19H12O8

Storage (From the date of receipt)
CAS No. 13739-02-1 Download SDF Storage of Stock Solutions

Synonyms N/A SMILES CC(=O)OC1=CC=CC2=C1C(=O)C3=C(C2=O)C=C(C=C3OC(=O)C)C(=O)O

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Mechanism of Action

In vitro
Diacerein significantly inhibits LPS-induced IL-1beta production by synovial tissue and cartilage. This compound (1 μM) has a significantly less inhibitory effect on cartilage synthesis than culture media containing LPS only. It decreases NO release in synovial tissue and cartilage media and increases IL-1ra levels in cartilage culture media. This chemical (10 μM) enhances the expression of TGF-beta1 and TGF-beta2 in cultured bovine articular chondrocytes. It reduces, in a dose-dependent manner, the interleukin-1-beta (IL-1beta)-induced MMP-13 production in osteoarthritic subchondral bone. This agent significantly reduces the activity of MMP-13 and cathepsin K in osteoclasts. It effectively blocks the IL-1beta effect on the osteoclast differentiation process and the survival of mature osteoclasts.
In vivo
Diacerein (100 mg/kg/day) significantly suppresses the paw edema and the increase in serum mucoprotein in the adjuvant-induced arthritic rats. This compound (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. It (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. This chemical (25 mg/kg) decreases the thickness of cartilage and subchondral bone in the lesion (middle) zone of the lateral tibial plateau in Merino wethers.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/12126975/
  • [5] https://pubmed.ncbi.nlm.nih.gov/11327258/

Applications

Methods Biomarkers Images PMID
Western blot Cyclin B1 / CDK1 / CDK2 AKT / p-AKT / p38 / p-p38 / p53 p-STAT3 / STAT3 MDM2 / CDC2
S4267-WB1
26555773

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-01-20)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07352306 NOT_YET_RECRUITING
Psoriasis Vulgaris
Cairo University
2026-02-01 PHASE4
NCT04318041 RECRUITING
Knee Osteoarthritis
TRB Chemedica
2020-11-22 PHASE3
NCT07199933 NOT_YET_RECRUITING
MAFLD
Hongyan Wu
2025-10-01
NCT06073132 ACTIVE_NOT_RECRUITING
Generalized Epidermolysis Bullosa Simplex
TWi Biotechnology, Inc.
2024-04-04 PHASE2; PHASE3
NCT07549386 COMPLETED
Pain Management; Osteoarthritis
Laboratorios Liomont
2024-05-24 PHASE3
NCT06912035 COMPLETED
Uncontrolled Diabetes; Diabetes Mellitus Type 2
Universitas Sriwijaya
2024-06-21 PHASE2; PHASE3

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