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他克莫司一水合物 |
| CAS No.: |
109581-93-3 |
| 分子式： |
C44H69NO12 |
| 分子量： |
804.02 |
| 备注： |
中文名称他克莫司一水合物中文同义词他克莫司一水合物;FK-506一水合物;他克莫司,一水;他克莫司水合物;他克莫司USP标准品;(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26AS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26A-十六氢-5,19-二羟基-3-[(1E)-2-[(1R,3R,4R)-4-羟基-3-甲氧基环己基]-1-甲基乙烯基]-14,16-二甲氧基-4,10,12,18-四甲基-8-(2-丙烯基-1-基)-15,19-环氧-3H-吡啶并[2,1-C][1,4]氧杂氮杂环二十三烯-1,7,20,21(4H,23H)-四酮一水合物;他克莫司对照品带水;他克莫司一水物英文名称TacrolimusMonohydrate英文同义词FK-506;15,19-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone,5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-,monohydrate,[3S-[3R*[E(1S*,3S*,4S*)],4S*,5R*,8S*,9E,12R*,14R*,15S*,16R*,18S*,19S*,26aR*]]-;TACROLIMUSHYDRATE/TSUKUBAENOLIDEHYDRATE;(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-Hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)tetrone;Tacrolimus(150mg);(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-Hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-Methoxycyclohexyl]-1-Methylethenyl]-14,16-diMethoxy-4,10,12,18-tetraMethyl-8-(2-propen-1-yl)-;Tacrolimusmonohydrate;FK-506monohydrate,>=98%CAS号109581-93-3分子式C44H71NO13分子量822.05EINECS号617-559-7相关类别他克莫司杂质;医用原料;发酵类;医药原料;化学连接;原料药;抗生素;医用原料;化学试剂;化工原料;原料;精细化工原料;SignallingMol文件109581-93-3.mol结构式他克莫司一水合物性质熔点127-129°比旋光度D23-84.4°(c=1.02inchloroform)储存条件-20°C溶解度DMSO：可溶，20mg/mL形态粉末颜色白色到近乎白色Merck14,9025InChIKeyNWJQLQGQZSIBAF-MLAUYUEBSA-N他克莫司一水合物用途与合成方法生物活性Tacrolimusmonohydrate(FK506monohydrate)是大环内酯类化合物，Tacrolimusmonohydrate与FK506结合蛋白(FKBP)结合形成复合物并抑制钙调神经磷酸酶(calcineurinphosphataChemicalbookse)，从而抑制T淋巴细胞信号转导和IL-2转录。具有强免疫抑制特性。靶点PP2B(calcineurinphosphatase)Autophagyinducer体外研究Tacrolimusmonohydrate(FK506monohydrate;Fujimycinmonohydrate;FR900506monohydrate)inhibitscalcium-dependentevents,suchasIL-2genetranscription,NOsynthaseactivation,celldegranulation,andapoptosis.TacrolimusalsopotentiatestheactionsofglucocorticoidsandprogesteronebybindingtoFKBPscontainedwithinthehormonereceptorcomplex,preventingdegradation.TheagentmayenhanceexpressionoftheTGFβ-1geneinafashionanalogoustothatdemonstratedforCsA.TcellproliferationinresponsetoligationoftheTcellreceptorisinhibitedbyTacrolimus.TreatmentwithalowconcentrationofTacrolimus(FK506,10μg/L)doesnotsignificantlyaffecttheproliferationofMH3924Acells(P=0.135).UpontreatmentwithhigherconcentrationsofTacrolimus(100-1,000μg/L),theproliferationofMH3924Acellsissignificantlyenhanced(P<0.01).TreatmentwithAMD3100atanyconcentration(10,50or100μg/L),hasnoobviouseffectonMH3924Acellproliferation(P>0.05).However,whendifferentconcentrationsofAMD3100arecombinedwith100μg/LTacrolimus,theinvitroproliferationofMH3924Acellsisincreased(P<0.01).体内研究ThetherapeuticeffectofTacrolimusisinvestigatedonprogressionandperpetuationofcolitisbyadministeringTacrolimustoDextransulfatesodium(DSS)-treatedmicefromDays10to16orto23.AtDays17and24,colonlengthissignificantlyshortened,andcolonweightissignificantlyhigherinDSS-treatedcontrolanimalsthaninnormalanimals.Inaddition,colonweightperunitlengthinthecontrolgroupismorethantwicethatinthenormalgroup.Whileboth7and14dtreatmentwithTacrolimussignificantlysuppressesincreasesincolonweightperunitlengthinDSS-treatedanimalscomparedwiththecontrolgroup,thistreatmentdoesnotactuallyrestorethecolonshortening.Inaddition,thisinhibitoryeffectofTacrolimusonincreasesincolonweightperunitlengthismorepronouncedwith14-dthan7-dtreatment,asshownbytheinhibitorypercentages(59%vs.28%). |
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