中文名称佛波醇12-十四酸酯13-乙酸酯中文同义词乙酸佛波酯;乙酸佛波酯PMA;豆蔻酰佛波醇乙酯;佛波脂酸(5MG/ML);TISSUEPLASMINOGENACTIVATOR人;佛波酯;12-十四酸酯13-乙酸佛波醇酯;12-O-十四烷酰佛波醋酸酯-13英文名称PHORBOL12-MYRISTATE13-ACETATE英文同义词13-o-acetylphorbol12-myristate;4)benz(1,2-e)azulen-5-one9a-acetate,(+)-ethyl-5h-cyclopropa(;5h-cyclopropa(3,4)benz(1,2-e)azulen-5-one,1,1a-beta,1b-alpha,4,4a,7a-beta,7b,;12-O-Tetradecanoyl-Phorbol-13-Acetate(TPA,MPA)16561-29-8;12-O-tetradecanoylphorbol-13-acetate(PMA);Phorbol-12-myristate-13-acetate-CAS16561-29-8-Calbiochem;InSolutionPhorbol-12-myristate-13-acetate-CAS16561-29-8-Calbiochem;4BETA-PHORBOL12-MYRISTATE13-ACETATECAS号16561-29-8分子式C36H56O8分子量616.83EINECS号605-413-5相关类别标准品;精细化工;对照品;生化试剂;对照品-中药对照品;抗体-二抗;重组蛋白;通用生化试剂-脂类;带图片的产品;Activator;enzyme;chemicalreagent;pharmaceuticalintermediate;ProteinKinase;Signalling;phytochemical;referencestandardsfromChinesemedicinalherbs(TCM).;standardizedherbalextract;DiterpenoidsMol文件16561-29-8.mol结构式佛波醇12-十四酸酯13-乙酸酯性质熔点65-79oC沸点571.87°C(roughestimate)密度1.17±0.1g/cm3(20ºC760Torr)折射率1.4900(estimate)储存条件-20°C溶解度可溶于DMSO,DMSO溶液可以在20℃下避光保存至少六个月。酸度系数(pKa)11.19±0.70(Predicted)形态精细结晶粉末颜色灰白色至浅黄色水溶解性Verysolubleinmethanol,solubleinDMSO,chloroform,ethanoloracetone,ether,ethylacetate,DMForacetonitrile.Insolubleinwater.敏感性LightSensitiveBRN2407201稳定性可在-20°下的DMSO或乙醇溶液保存长达2个月。InChIKeyPHEDXBVPIONUQT-RGYGYFBISA-NCAS数据库16561-29-8(CASDataBaseReference)EPA化学物质信息12-O-Tetradecanoylphorbol13-acetate(16561-29-8)佛波醇12-十四酸酯13-乙酸酯用途与合成方法佛波酯佛波酯又称佛波醇酯、大戟二萜醇酯,是巴豆油中的成分,十四烷酸和佛波醇形成的酯。已证实是一种促癌剂。其促癌活性大小不一,活性最高的是12-邻十四烷酰大戟二萜醇-13-乙酸酯(TPA),其余依次为大戟二萜醇-12,13-双癸酸酯、大戟二萜醇-12,13-双丁酸酯、4-邻甲基大戟二萜酸-12-十四烷酰-13-乙酸酯、大戟二萜醇-12,13-双癸酸酯。促癌机制不很清楚,近期认为与启动细胞膜相互作用,促进第二信使Chemicalbook的合成和增加蛋白激酶活性有关。佛波酯能激活导致细胞增殖或分化的信号通路而具有促进细胞癌变的作用。其中活性最高的是12-邻-14-烷酰佛波醇-13-乙酸酯。生物活性Phorbol12-myristate13-acetate(PMA,12-O-Tetradecanoylphorbol-13-acetate,TPA)是一种有效的PKC激活剂,在纳摩尔浓度范围内具有活性作用。Phorbol12-myristate13-acetate(PMA)可诱导sphingosine-1-phosphate(S1P)。靶点PKC11.7nM(EC50)体外研究InordertoexaminetheroleofPKCinp38MAPKphosphorylation,thecellsarestimulatedwiththePKCactivator,PMA(100nM),whichmimicsthebindingofDAG,thenaturalactivatorofPKC,totheC1regionofthePKCs.p38MAPKphosphorylationbyPMAisobservedinthetwocelltypessimilartothatobservedbyGnRHinαT3-1cells,thatis,aslowsustainedactivation(3.2-foldand3.6-fold,respectivelyat30min).TheparadoxicalfindingsthatPKCsactivatedbyGnRHandPMAplayadifferentialroleinp38MAPKphosphorylationmaybeexplainedbydifferentiallocalizationofthePKCs.Basal,GnRH-andPMA-stimulationofp38MAPKphosphorylationinαT3-1cellsismediatedbyCa2+influxviavoltage-gatedCa2+channelsandCa2+mobilization,whileinthedifferentiatedLβT2gonadotropecellsitismediatedonlybyCa2+mobilization.THP-1cellsaredifferentiatedintomacrophage-likecells(THP-1macrophages)byincubationinthepresenceofPMA(200ng/mL;1-5days),whichleadstoamacrophage-likephenotypecharacterizedbychangesinmorphologyandincreasedcellsurfaceexpressionofCD11andCD14.InthemonocyticcelllineTHP-1,PMAresultsinamoredifferentiatedphenotypethanVD3,accordingtoadherence,lossofproliferation,phagocytosisoflatexbeads,andexpressionofCD11bandCD14.体内研究PMAisaPKCagonist,whichreversesthedamageinducedby5-hydroxydecanoicacid(5-HD).Thus,activationofthemitoKATPprotectedmitochondrialfunctioninSODandMDAviathePKCpathway.类别有毒物品毒性分级剧毒急性毒性静脉-小鼠LD50:0.309毫克/公斤可燃性危险特性可燃,火场排出辛辣刺激烟雾储运特性库房通风低温干燥;与食品分开储运灭火剂水,砂土,泡沫 |