Diacerein,13739-02-1

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产品名称：Diacerein

产品别名：1,8-二乙酰基-3-羧基蒽醌

英文别名：Diacerhein;Diacetylrhein;Fisiodar;Artrodar

靶点：Interleukin Related

CAS：13739-02-1

纯度：98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

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

溶解性：DMSO：48mg/ml(130.33 mM)

体外研究：

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.

体内研究：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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