product name Diacerein
Description: Diacerein is a potent inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, it is indicated 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.
References: Osteoarthritis Cartilage. 1999 May;7(3):272-80; Osteoarthritis Cartilage. 1999 May;7(3):255-64.
368.29
Formula
C19H12O8
CAS No.
13739-02-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 48 mg/mL (130.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
1% CMC Na: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
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| 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. |
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| References | Osteoarthritis Cartilage. 1999 May;7(3):272-80; Osteoarthritis Cartilage. 1999 May;7(3):255-64; Eur J Pharmacol. 2002 Jul 12;448(1):81-7; J Rheumatol. 2001 Apr;28(4):825-34. |
