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WAY-362450以3mg\u002Fkg(口服和静脉注射)给予大鼠,并显示出良好的口服生物利用度(38％)。延长半衰期为25小时,分布容积适中,清除率低(3.3 L\u002Fkg,肝血流量约10％)。小鼠和高等物种的其他药代动力学研究已经完成,数据将在其他地方报道[1]。在大鼠中,WAY-362450导致HDLc水平升高,而在仓鼠中它导致类似于在小鼠中观察到的降低[2]用30mg\u002Fkg WAY-362450处理野生型小鼠导致SHP表达的诱导。在野生型小鼠中,但在FXR -\u002F-小鼠中没有。与SHP诱导对胆汁酸合成基因表达的已知作用一致,WAY-362450强烈抑制CYP8B1胆汁酸合成基因在野生型小鼠中的表达,但对FXR -\u002F-小鼠中的CYP8B1基因表达没有影响[3]。 。",{"key":250,"value":251},"细胞实验","将小鼠AML12细胞以200,000个细胞\u002F孔接种在24孔板上的1mL生长培养基中[DMEM \u002F F12 10％FBS，1％青霉素和链霉素，1％胰岛素 - 转铁蛋白 - 硒-G补充剂（ITS）， 0.1％地塞米松（40 ng \u002F mL）\u002F孔。用递增浓度的WAY-362450（0.001,0.01,0.1,1和10μM）或GW4064处理细胞24小时。通过实时RT-PCR制备和分析总RNA，并将短异二聚体配偶体（SHP）表达标准化为GAPDH并报告为诱导倍数与媒介物处理的细胞。从Cellz Direct获得具有基质胶覆盖层的预先植入的具有基质胶覆盖的人雄性原代肝细胞的24孔板。将细胞维持在无血清Williams培养基E中并补充青霉素\u002F链霉素，地塞米松，ITS，L-谷氨酰胺和HEPES缓冲液。用载体（0.01％DMSO）或递增浓度的WAY-362450或GW4064处理它们过夜。使用Qiagen RNeasy清洁试剂盒纯化总RNA，并使用ABI 7900，使用Qiagen Quantitech试剂盒通过实时RT-PCR定量基因表达。将mRNA的相对量标准化为18S核糖体RNA，并且显示的数据代表平均两次独立实验[2]。",{"key":253,"value":254},"动物实验","小鼠[3]年龄和性别匹配的8至12周龄小鼠喂食标准食物，并在温度控制无病毒的设施中饲养12小时光照\u002F黑暗循环，可自由获取食物和水。在指出的情况下，给小鼠喂食含有42％脂肪和0.2％重量胆固醇的西方饮食，或者补充这种西方饮食，每克饮食含有0.225mg WAY-362450。假设体重为30g，小鼠每天消耗~4g饮食，导致每公斤体重输送~30mg WAY-362450。动物在这些饮食中维持6（apoE  -  \u002F  - ）或12周（LDLR  -  \u002F  - ）。在每次研究结束时，对动物实施安乐死并通过眼眶眼收集血样用于脂质分析。取出肝脏和回肠组织用于mRNA定量，取出主动脉并储存在10％缓冲的福尔马林溶液中。大鼠[2]给8周龄雄性Sprague Dawley大鼠和叙利亚金仓鼠喂食60％果糖\u002F0.15%胆固醇饮食。对于大鼠研究，将大鼠置于饮食上2周，然后通过每天口服管饲法用载体（80％聚乙二醇\u002F 20％吐温）或不同浓度的WAY-362450（8 \u002F组）进行治疗，如7所示。天（8只大鼠\u002F组）。仓鼠研究是作为预防性治疗进行的，因此饮食和药物治疗均在第1天开始并持续21天（8只仓鼠\u002F组）。在最终剂量后的最后一天，取出食物以禁食3小时，并如上所述收获血清和肝脏用于分析。",{"key":256,"value":257},"参考文献","[1].\nFlatt B, et al. 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