| CAS NO: | 13739-02-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 25mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
| 250mg | 询价 |
| 500mg | 询价 |
| 1g | 询价 |
| Molecular Weight (MW) | 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 | Diacerhein; Diacetylrhein; DAR; SF 277 |
| 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. |
|---|---|
| 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. |
| Animal model | Rats |
| Formulation & Dosage | 30, 100 mg/kg |
| 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. |
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