Diacerein

製品コードS4267 バッチS426702

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C19H12O8

分子量 368.29 CAS No. 13739-02-1
Solubility (25°C)* 体外 DMSO 18 mg/mL (48.87 mM)
Water Insoluble
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.
in vitro Diacerein significantly inhibits LPS-induced IL-1beta production by synovial tissue and cartilage. This compound (1 μM) has a significantly less inhibitory effect on cartilage synthesis than culture media containing LPS only. It decreases NO release in synovial tissue and cartilage media and increases IL-1ra levels in cartilage culture media. [1] This chemical (10 μM) enhances the expression of TGF-beta1 and TGF-beta2 in cultured bovine articular chondrocytes. [2] It reduces, in a dose-dependent manner, the interleukin-1-beta (IL-1beta)-induced MMP-13 production in osteoarthritic subchondral bone. This agent significantly reduces the activity of MMP-13 and cathepsin K in osteoclasts. It effectively blocks the IL-1beta effect on the osteoclast differentiation process and the survival of mature osteoclasts. [3]
in vivo Diacerein (100 mg/kg/day) significantly suppresses the paw edema and the increase in serum mucoprotein in the adjuvant-induced arthritic rats. This compound (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. It (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] This chemical (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]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/10329302/
  • https://pubmed.ncbi.nlm.nih.gov/10329300/
  • https://pubmed.ncbi.nlm.nih.gov/18578867/
  • https://pubmed.ncbi.nlm.nih.gov/12126975/
  • https://pubmed.ncbi.nlm.nih.gov/11327258/

カスタマーフィードバック

, , J Neuroinflammation, 2016, 13(1):183.

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Autophagy-mediated activation of the AIM2 inflammasome enhances M1 polarization of microglia and exacerbates retinal neovascularization [ MedComm (2020), 2024, 5(8):e668] PubMed: 39081514
Combination of hyperlipidemia and 17β-Estradiol induces TMJOA-like pathological changes in rats [ Oral Dis, 2022, 10.1111/odi.14294] PubMed: 35765240
Peroxynitrite activates NLRP3 inflammasome and contributes to hemorrhagic transformation and poor outcome in ischemic stroke with hyperglycemia [ Free Radic Biol Med, 2021, 165:171-183] PubMed: 33515754
Deletion of Glutathione S-Transferase Omega 1 Activates Type I Interferon Genes and Downregulates Tissue Factor [ Cancer Res, 2020, canres.530.2020] PubMed: 32571799
Small molecule inhibitor of TAK1 ameliorates rat cartilaginous endplate degeneration induced by oxidative stress in vitro and in vivo. [ Free Radic Biol Med, 2020, 148:140-150] PubMed: 31911149
Chemokine CXCL13 mediates orofacial neuropathic pain via CXCR5/ERK pathway in the trigeminal ganglion of mice [Zhang Q, et al. J Neuroinflammation, 2016, 13(1):183] PubMed: 27401148

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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