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Property","更多","1.熔点：146-147℃。",null,[],[246,249,252,255,258],{"key":247,"value":248},"描述","舍他康唑(FI7056游离碱)是一种广谱局部抗真菌剂,通过激活p38-COX-2-PGE2途径发挥抗炎活性。舍他康唑也是一种微管抑制剂,具有抗增殖作用,诱导细胞凋亡和自噬,还可以抑制细胞迁移[1][2][3][4]。",{"key":250,"value":251},"相关类别","信号通路\n>>\n细胞凋亡\n>>\n细胞凋亡\n研究领域\n>>\n癌症\n研究领域\n>>\n感染\n信号通路\n>>\n抗感染\n>>\n真菌\n信号通路\n>>\n细胞周期\u002FDNA损伤\n>>\n微管\u002F微管蛋白\n信号通路\n>>\n自噬\n>>\n自噬\n信号通路\n>>\nMAPK\u002FERK信号通路\n>>\np38 MAPK\n研究领域\n>>\n炎症\u002F免疫\n信号通路\n>>\n细胞骨架\n>>\n微管\u002F微管蛋白",{"key":253,"value":254},"体外研究","Sertaconazole(0.03-40µg\u002FmL；24小时)抑制150株酵母菌,其中包括六种念珠菌,算术平均MIC为0.77µg\u002FmL[1]。舍他康唑(1µg\u002FmL；5、10、30、60分钟)以时间依赖性方式激活p38 MAP激酶[2]。Sertaconazole(1,2µg\u002FmL；6,8或24小时)通过COX-2在角质形成细胞中增加PGE2的两倍释放,这依赖于p38激活[2]。西康唑(10、20、30、40µM；24小时)通过解聚间期微管和纺锤体微管,诱导强烈的有丝分裂阻滞,从而诱导染色体聚集缺陷并产生抗增殖作用[3]。Sertaconazole(20,40µM；24小时)通过p53途径诱导HeLa细胞凋亡[3]。Sertaconazole(20、30µM；24、48和72小时)以浓度依赖性方式抑制HeLa细胞的迁移[3]。舍他康唑(15,30µM；24小时)诱导A549、H460细胞自噬[4]。细胞存活率测定[1]细胞系：白念珠菌、吉列蒙念珠菌、克鲁西念珠菌、副硅氧烷、热带念珠菌、无毛念珠菌浓度：0.03-40µg\u002Fm孵育时间：24小时结果：对150株酵母菌(六种念珠菌),其中包括白念珠菌,吉列蒙弧菌、克鲁斯弧菌、副西罗弧菌、热带念珠杆菌、无毛弧菌,其算术平均MIC值分别为1.02、0.51、0.38,分别为0.31、1.67和0.78µg\u002FmL。Western印迹分析[2]细胞系：HaCaT细胞浓度：1µg\u002FmL孵育时间：5、10、30、60分钟结果：显示p38 MAP激酶和Hsp27的激活活性呈时间依赖性。Western印迹分析[2]细胞系：HaCaT细胞浓度：1,2µg\u002FmL孵育时间：6或8小时结果：诱导COX-2表达50%,导致PGE2释放增加两倍。Western印迹分析[2]细胞系：siRNA转染的HaCaT细胞(无p38 MAP激酶表达)浓度：1µg\u002FmL孵育时间：24小时结果：介导的PGE2诱导依赖于p38激活。细胞增殖试验[3]细胞系：HeLa、HEK-293、MCF-7、A549细胞浓度：0-100µM孵育时间：24小时结果：显示抗增殖活性,对HeLa,HEK-29 3、A549和MCF-9细胞的IC50分别为38、45.1、41.5和40.8µM。在浓度超过30μM时表现出有丝分裂阻滞活性和诱导细胞死亡,但有丝分裂细胞数量没有显著增加。解聚的间期微管和纺锤体微管导致染色体一致性缺陷。凋亡分析[3]细胞系：HeLa细胞浓度：10、20、40µM孵育时间：24小时结果：在浓度为10、20和40μM时,分别诱导约5%、10%和21%的细胞凋亡。Western Blot分析[3]细胞系：A549细胞浓度：20,40µM孵育时间：24小时结果：通过p53途径诱导凋亡,p53表达分别从30%到50%和95%,p21表达分别从11%到39%和40%。导致p53的两个直接转录靶标Noxa和Puma过度表达。细胞迁移试验[3]细胞系：HeLa细胞浓度：20、30µM孵育时间：24、48和72 h结果：在低于其IC50的浓度下抑制HeLa的迁移,其浓度依赖性。细胞自噬测定[4]细胞系：A549、H460细胞浓度：15、30µM孵育时间：24小时结果：内源性LC3点状细胞和LC3强度增加,这表明A549和H460中诱导了自噬。",{"key":256,"value":257},"体内研究","舍他康唑(1%(w\u002Fv)；应用于左耳一次)抑制TPA诱导的CD-1小鼠耳水肿[2]。动物模型：CD-1小鼠(TPA诱导的耳水肿模型)[2]。剂量：1%(w\u002Fv)给药：应用于左耳,一次。结果：通过介导PGE2的释放,小鼠的炎症反应明显减轻。",{"key":259,"value":260},"参考文献","[1].\nCarrillo-Muñoz AJ, et al. In-vitro antifungal activity of sertaconazole, econazole, and bifonazole against Candida spp. J Antimicrob Chemother. 1995 Oct;36(4):713-6.\n[2].\nSur R, et al. Anti-inflammatory activity of sertaconazole nitrate is mediated via activation of a p38-COX-2-PGE2 pathway. J Invest Dermatol. 2008 Feb;128(2):336-44.\n[3].\nSebastian J, et al. Sertaconazole induced toxicity in HeLa cells through mitotic arrest and inhibition of microtubule assembly. Naunyn Schmiedebergs Arch Pharmacol. 2021 Jun;394(6):1231-1249.\n[4].\nZhang W, et al. Sertaconazole provokes proapoptotic autophagy via stabilizing TRADD in nonsmall cell lung cancer cells. MedComm (2020). 2021 Dec 16;2(4):821-837.",[262,268],{"slug":263,"cid":264,"name":265,"nameZh":265,"cas":266,"imgSvg":267},"785892912771633200","J-1494141-4","3-溴甲基-7-氯苯并[B]噻吩","17512-61-7","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F090\u002F17512-61-7.svg",{"slug":269,"cid":270,"name":271,"nameZh":271,"cas":272,"imgSvg":273},"785881294813794300","J-1051732-9","1-(2,4-二氯苯基)-2-...","24155-42-8","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F191\u002F24155-42-8.svg",[],[],[277,280,283,286],{"key":278,"value":279},"危害码 (欧洲)","Xi",{"key":281,"value":282},"安全声明 (欧洲)","S22-S24\u002F25",{"key":284,"value":285},"WGK德国","2",{"key":287,"value":288},"RTECS号","KM6557000","\u003Ctd>\n\n\u003Cp>\u003Ca href=\"\u002Fen\u002Fcas\u002F99592-32-2_1026706.html#duXinDiv\">舍他康唑毒性英文版\u003C\u002Fa>\u003C\u002Fp>\n\n\u003C\u002Ftd>","\u003Cp> 在氮气保护下，将氢化钠(约50%) (1.60mmol)用六甲基磷酰胺(HMPT)(3×5m1)洗3次。在0℃和剧烈搅拌下，加入化合物(I)(0.372g，1.45mmo1)(其制备可参见Godefroi E F，et a1．J Med Chem，1969，12：784)在5ml六甲基磷酰胺的溶液，在0℃下搅拌至氢气放出停止，再在50℃下搅拌1h。冷至0℃，在搅拌下，缓慢加入溶于5ml六甲基磷酰胺的2-(溴甲基)苯并[b]噻吩(0.42g，1.60mmo1)(其制备参见Cuberes M．Et a1.Magn Reson Chem，1985，23：814)，在室温下搅拌5h。加入乙醚和水进行分配。分出有机层，水洗，干燥，浓缩。剩余物用硅胶层析提纯，得舍他康唑，收率62%，熔点146-147℃。 \u003C\u002Fp>","2026-08-21T07:51:12.859463Z",false,[294,300,306,312,317,323],{"slug":295,"cid":296,"name":297,"nameZh":298,"cas":299},"785875705589141504","J-10742-4","Neocuproine hemihydrate","新亚铜试剂半水合物","34302-69-7",{"slug":301,"cid":302,"name":303,"nameZh":304,"cas":305},"785898367673700352","J-1988074-7","Pantoprazole Sodium Sesquihydrate","泮托拉唑钠倍半水合物","164579-32-2",{"slug":307,"cid":308,"name":309,"nameZh":310,"cas":311},"785882335940710400","J-3147-5","Pigment Red 57:1","颜料红57:1","5281-04-9",{"slug":313,"cid":314,"name":315,"nameZh":315,"cas":316},"785947418393841664","J-1874835-6","((Perfluorohexyl)ethyl)-2-chloropropenoate","96383-55-0",{"slug":318,"cid":319,"name":320,"nameZh":321,"cas":322},"785889757879078912","J-1372965-3","Calcium Saccharin Hydrate","糖精钙水合物","6381-91-5",{"slug":324,"cid":325,"name":326,"nameZh":327,"cas":328},"785891221192052736","J-1095551-6","Sudan Black B","苏丹黑B","4197-25-5",1792669194439,"zh-CN",[]]