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Diacerein

Name: Diacerein
Brand: Selleck Chemicals
SKU: S4267
Rating: 5 (5 reviews)

Catalog No.S4267 Purity: 99.25%

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

Diacerein Chemical Structure

CAS: 13739-02-1

Selleck's Diacerein has been cited by 5 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.25%

99.25

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

In Vivo
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT03472287	Completed	Epidermolysis Bullosa (EB)\|Epidermolysis Bullosa Simplex\|Dystrophic Epidermolysis Bullosa\|Junctional Epidermolysis Bullosa	Castle Creek Pharmaceuticals LLC	May 18 2018	Phase 1

References

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Chemical lnformation & Solubility

Molecular Weight	368.29	Formula	C₁₉H₁₂O₈
CAS No.	13739-02-1	SDF	Download Diacerein SDF
Smiles	CC(=O)OC1=CC=CC2=C1C(=O)C3=C(C2=O)C=C(C=C3OC(=O)C)C(=O)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 18 mg/mL ( (48.87 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh 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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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.

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