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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|Description||Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.|
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.  Diacerein (10 μM) enhances the expression of TGF-beta1 and TGF-beta2 in cultured bovine articular chondrocytes.  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. 
|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.  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. |
-  Yaron M, et al. Osteoarthritis Cartilage, 1999, 7(3), 272-280.
-  Felisaz N, et al. Osteoarthritis Cartilage, 1999, 7(3), 255-264.
-  Boileau C, et al. Arthritis Res Ther, 2008, 10(3), R71.
|In vitro||DMSO||48 mg/mL (130.33 mM)|
|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.
* 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.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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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|
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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