Licofelone

Licofelone

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  • ¥600 - 3200
  • 上海莼试
  • CS-01Y76435
  • 国产
  • 2025年07月12日
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    • 详细信息
    • 技术资料
    • 库存

      56

    • 英文名

      Licofelone

    • CAS号

      156897-06-2

    • 供应商

      上海莼试

    • 保存条件

      Store at -20°C

    • 规格

      10mM (in 1mL DMSO) 5mg 50mg

    商品属性:
    货号 CS-01Y76435 规格 10mM (in 1mL DMSO) 5mg 50mg
    CAS号 156897-06-2 分子量 379.88
    含量 >98.00% 别名  
    分子式 C23H22ClNO2 化学名 2-[2-(4-chlorophenyl)-6,6-dimethyl-1-phenyl-5,7-dihydropyrrolizin-3-yl]acetic   acid
    产地 国产 用途 仅供科研研究实验
    产品描述:
    分子式:C23H22ClNO2

    Licofelone
    分子量:379.88
    溶解度:≥ 6.3mg/mL in DMSO with gentle warming
    储存条件:Store at -20°C
    General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the   ultrasonic bath for a while.
    Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or   blue ice upon request                                      
    IC50: Inhibitor of COX-1, COX-2 and 5-LOX with IC50 values of 0.16 M, 0.37 M and 0.23 M respectively in human.Licofelone (ML3000), developed by the German pharmaceutical company - Merckle GmbH, is a potent suppressor of both COX and LOX. As the first member of this new class of analgesic and anti-inflammatory drugs, Licofelone is suggested as a novel treatment for osteoarthritis (OA), the most common form of arthritis. [1]In vitro: The 5-LOX and COX inhibitory effect of licofelone was firstly identified via bovine thromobocyte intact cell assay and intact bovine PMN leukocytes. Licofelone was also reported to inhibit PGE2 in a dose-dependent manner in human whole blood assay. Moreover, Licofelone was found to suppress in vitro generation of reactive oxygen species and to reduce release of elastase from PMN leukocytes. All above findings revealed that Licofelone had an inhibitory effect on COX-1/-2 and 5-LOX. [1]In vivo: The pharmacodynamic properties of Licofelone were evaluated in various animal models and compared with those of commonly used NSAIDs. Based on studies from a rat model of incisional pain, orally administration of Licofelone had a longer duration of action and was more effective than indomethacin and zileuton. [1]Clinical trials: Two double-blind phase-II studies had been conducted to detect the efficacy of licofelone in OA. In the first study, 107 patients were treated with different doses of licofelone or placebo for 4 weeks. It was reported that licofelone at 200 or 400 mg twice a day could significantly ameliorate the symptoms of OA. In the second study, licofelone at doses of 100, 200 and 400 mg was administered to 404 patients twice a day, WOMAC pain subscore showed a notable decrease of 37%, 40% and 42% respectively. Licofelone at 400 mg twice a day was found to cause adverse events including diarrhea and abdominal pain. [1]
    注意事项:
    抗逆滴加序列
    每次向板内滴加抗原时,移液器滴头要与平面45度悬空,不要触碰到孔内的液体,由后向前依次滴加(即浓度由低往高滴加)。
    抗感染反应期
    抗原抗体在室温20~25℃下,必须反应30min以上,若环境温度低于室温,可将微量反应板置于恒温培养箱中,使二者充分反应。
    旅游温度
    磷酸盐缓冲液的pH值要在高压灭菌后进行滴定,往往在高压后pH值会有所改变,所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时,红细胞会产生自凝现象;当pH>7.8时,图形洗脱加快,易造成肉眼观察产生误差;p H=7.2时,红细胞沉降最充分,图形最清晰。
    当滴注 1%红细胞悬液时,应经常摇晃红细胞悬液,使红细胞均匀地分布在磷酸缓冲液中,以防止红细胞下降。
    反应时间及温度
    加入鸡红血球之后,反应板在室温(20~25℃)静置30~40min,对照孔血球下沉于孔底,即可判定结果。若室温达不到实验要求,需相应调整反应时间。当环境温度低于4℃时,红细胞发生自凝;高于37℃时,会发生反应物分离和红细胞溶血。
    使用方法:
    1.本蛋白酶抑制剂混合物为100×的储存液,使用时按照1:100的比例加入到裂解液中(例如,1ml裂解液中加入10μl蛋白酶抑制剂混合物),混匀后即可使用。根据需要,0.5M的EDTA也按照1:100的比例加入到裂解液中(如用于检测金属蛋白酶活性,则不宜添加EDTA)。含有蛋白酶抑制剂混合物的裂解液宜现用现配,不宜配制后冻存待后续使用。
    2. 待所需的抑制剂添加完毕混匀后,就可以开始进行哺乳动物组织的裂解和蛋白提取。
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