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当前位置: 首页 > 信号通路研究 > COX > Rofecoxib
Rofecoxib
Rofecoxib
Rofecoxib
商品货号:MB8193
CAS 号:162011-90-7
英文名字:Rofecoxib
质量标准:>98%,COX-2抑制剂
分子式:C17H14O4S
  • 包装规格:
    规格 库存 发货时间
    50MG [¥380.00]15 现货
    200MG [¥900.00]15 现货
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    商品信息

    质检证书(coa)

    说明书下载

    Rofecoxib

    分子式:C17H14O4S   分子量:314.36

    相关谱图:

    HNMR | HPLC

    产品描述

    Rofecoxib (Vioxx)COX-2抑制剂,IC5018 nM

    靶点

    COX-2

             

    IC50

    18 nM

             

    体外研究

    Rofecoxib inhibits the COX-2-dependent production of PGE2 in human osteosarcoma cells with an IC50 of 26 nM. Rofecoxib is a time-dependent inhibitor of purified human recombinant COX-2 with an IC50 of 0.34 μM. Rofecoxib causes inhibition of purified human COX-1 in a non-time-dependent manner. In a human whole blood assay, Rofecoxib selectively inhibits lipopolysaccharide-induced, COX-2-derived PGE2 synthesis with an IC50 value of 0.53 μM compared with an IC50 value of 18.8 μM for the inhibition of COX-1-derived thromboxane B2 synthesis after blood coagulation.Rofecoxib moderately inhibits phenacetin O-deethylation with an IC50 of 23 μM. And a 30-minute preincubation with microsomes and NADPH considerably increases the inhibitory effect of Rofecoxib with an IC50 of 4.2 μM. Inactivation of CYP1A2 by rofecoxib requires NADPH, and is characterized by a K i of 4.8 μM.

    体内研究

    Rofecoxib potently inhibits carrageenan-induced paw edema, carrageenan-induced paw hyperalgesia, lipopolysaccharide-induced pyresis with IC50 of 1.5 mg/kg, 1.0 mg/kg and 0.24 mg/kg, respectively. Rofecoxib also blocks adjuvant-induced arthritis with an IC50 of 0.74 mg/kg/day. Rofecoxib also has a protective effect on adjuvant-induced destruction of cartilage and bone structures in rats.Oral administration of rofecoxib decreases portal pressure in rats that are treated with CCl4 for 8 weeks. In addition, rofecoxib administration reduces the number of activated HSCs and to downregulate hepatic protein levels of three detected types of collagen, laminin, VEGF and CTGF in CCl4-treated rats.

    溶解性

    DMSO 63 mg/mL,水 <1 mg/mL,乙醇 <1 mg/mL

    稳定性

    2 -20°C粉状,6-80°C溶于DMSO

    特征

             

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    http://www.meilune.com/article.php?id=374

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