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包装规格：25g in glass bottle
溶解性：溶于DMSO（20mg/mL 超声)
产品描述：基本信息 产品编号： R10326  产品名称： Rofecoxib CAS: 162011-90-7   储存条件 粉末 2-8℃ 四年     分子式： C17H14O4S 溶于液体 -80℃ 6个月 分子量： 314.36 -20℃ 1个月 化学名：  4-(4-METHANESULFONYL-PHENYL)-3-PHENYL-5H-FURAN-2-ONE Solubility (25°C)：   体外:   DMSO 63mg/mL (200.4mM) Ethanol Insoluble Water Insoluble 体内(现配现用): 30% PEG400+0.5% Tween80+5% propylene glycol 30mg/mL ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.1811mL 15.9053mL 31.8107mL 5mM 0.6362mL 3.1811mL 6.3621mL 10mM 0.3181mL 1.5905mL 3.1811mL 50mM 0.0636mL 0.3181mL 0.6362mL   生物活性 产品描述 一种有效的，可口服的COX-2特异性抑制剂。 靶点 COX-2 18nM   体外研究 Rofecoxib (MK-0966) is a potent and orally active inhibitor of COX-2,with IC50s of 26 and 18nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells,with a 1000-fold selectivity for COX-2 over COX-1 (IC50>50μM in U937 cells and >15μM in Chinese hamster ovary cells).Rofecoxib time dependently inhibits purified human recombinant COX-2 (IC50=0.34μM) but suppresses purified human COX-1 in a non-time-dependent manner that can only be observed at a very low substrate concentration (IC50=26μM at 0.1μM arachidonic acid concentration).Rofecoxib selectively inhibits lipopolysaccharide-induced,COX-2-derived PGE(2) synthesis with an IC50 value of 0.53±0.02μM compared with an IC50 value of 18.8±0.9μM for the inhibition of COX-1-derived thromboxane B(2) synthesis after blood coagulation.Rofecoxib (36μM) causes a cell proliferation of 68% in MPP89,of 58% in Ist-Mes-1 and 40% in Ist-Mes-2.MSTO-211H and NCI-H2452 treated with 36μM of Rofecoxib have a survival of 97% and 90% respectively.Rofecoxib (36μM) decreases COX-2 and mRNA levels in Ist-Mes-1,Ist-Mes-2 and MPP89 cell lines. 体内研究 Rofecoxib potently inhibits carrageenan-induced paw edema (ID50=1.5mg/kg),carrageenan-induced paw hyperalgesia (ID50=1.0mg/kg),lipopolysaccharide-induced pyresis (ID50=0.24mg/kg),and adjuvant-induced arthritis (ID50=0.74mg/kg/day) in rodent models.Rofecoxib also protects adjuvant-induced destruction of cartilage and bone structures in rats.In a 51Cr excretion assay for detection of gastrointestinal integrity in either rats or squirrel monkeys,rofecoxib shows no effect at doses up to 200mg/kg/day for 5 days.Rofecoxib (15mg/kg,i.p.) reduces the blood vessels attached to the internal limiting membrane (ILM) in mice.COX-2 and VEGF protein expressions,COX-2 mRNA and VEGF mRNA are also significantly decreased by Rofecoxib in ROP mice.   推荐实验方法(仅供参考) 激酶实验： 体外重组人COX-1 和 COX-2生物化学和药理学抑制研究试验 重组人COX-1和COX-2的微粒体制剂从牛痘病毒-COS-7细胞表达系统制备。重组人COX-1和COX-2在杆状病毒-Sf9细胞中表达，并将酶纯化。酶活性通过荧光检测测量还原剂共底物高香草酸氧化型的表型或氧消耗监测。HPLC试验，用于评估0.1μM花生四烯酸底物浓度下Rofecoxib对纯化COX-1的抑制，COX-2和Rofecoxib复合物化学计量的测定，酶抑制剂复合物在酶活性恢复后的解离速率常数，完整Rofecoxib从复合物中的恢复均如上进行。Rofecoxib HPLC分析的溶剂体系为15:85 MeOH/磷酸钾水溶液(1g/L)，以15%-75% MeOH线性梯度洗脱25分钟，在Novapak C18柱上以275nm检测。   细胞实验:   The anti-proliferative activity of single drug treatments is assessed in a monolayer culture condition by plating Ist-Mes-1,IstMes-2 and MPP89 cells in T25 flask.After 24h,DMSO (at the same final concentration of that present in medium with drugs),50μM gefitinib or 36μM Rofecoxib are added.The cells are then harvested at 48h after treatment and analyzed by western blot and RT-PCR to evaluate the effect of the drugs on expression and mRNA levels of EGFR and COX-2.The expression of the cell cycle arrest genes and p-AKT,AKT,p-ERK and ERK is detected by Western blot to assess the antiproliferative activity of the two drugs in isolation (25μM gefitinib or 4μM Rofecoxib) and in combination 25μM gefitinib+4μM Rofecoxib.   动物实验:   Mice Retinopathy of prematurity (ROP) is induced in C57BL/6J mice.The mice are randomly allocated into three experimental groups with 16 mice in each group:normal group-age-matched mice are maintained in room air from birth to P17 and are served as negative control;untreated ROP group-ROP is induced as described above without treatment and served as positive control;Rofecoxib-treated ROP group-ROP mice are treated daily with Rofecoxib (15mg/kg body weight,intraperitoneally) from P12 to P17.Rofecoxib is dissolved in a 0.5% aqueous methylcellulose solution before administration.
保存条件：2-8℃

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