CyclosporinAisanimmunosuppressiveagent,thatbindstothecyclophilinandtheninhibitscalcineurinwithIC₅₀of7nMinacell-freeassay,andiswidelyusedinorgantransplantationtopreventrejection.

IC50:7nM(calcineurin)

CyclosporinAbindstothecyclophilin(immunophilin)inTcells^[1],andformsaCyclophilin-CyclosporinAcomplexwhichinhibitscalcineurin^[2]. CyclosporinAinhibitscalcineurinwithIC₅₀of7nM^[3],thenblocksthenucleartranslocationofNF-AT^[4]. CyclosporinAalsoaffectsmitochondriabypreventingtheMTP(mitochondrialpermeABIlitytransitionpore)fromopeningwithanIC₅₀of39nM^[5]. 

CyclosporinAisanimmunosuppressiveagentthatiseffectivefollowingeitherparenteralororaladmiNISTrationinmice,ratandguineapigs^[6]. CyclosporinAisclinicallyusedinorgantransplantationtopreventrejection^[7]. 

• [1].HandschumacherRE,etal.Cyclophilin:aspecificcytosolicbindingproteinforcyclosporinA.Science.1984Nov2;226(4674):544-7.

  [2].LiuJ,etal.Calcineurinisacommontargetofcyclophilin-cyclosporinAandFKBP-FK506complexes.Cell.1991Aug23;66(4):807-15.

  [3].FrumanDA,etal.CalcineurinphosphataseactivityinTlymphocytesisinhibitedbyFK506andcyclosporinA.ProcNatlAcadSciUSA.1992May1;89(9):3686-90.

  [4].FlanaganWM,etal.NuclearassociationofaT-celltranscriptionfactorblockedbyFK-506andcyclosporinA.Nature.1991Aug29;352(6338):803-7.

  [5].NicolliA,etal.Interactionsofcyclophilinwiththemitochondrialinnermembraneandregulationofthepermeabilitytransitionpore,andcyclosporinA-sensitivechannel.JBiolChem.1996Jan26;271(4):2185-92.

  [6].BorelJF,etal.Effectsofthenewanti-lymphocyticpeptidecyclosporinAinanimals.Immunology.1977Jun;32(6):1017-25.

  [7].Williams,R,etal.Randomisedtrialcomparingtacrolimus(FK506)andcyclosporininpreventionofliverallograftrejection.EuropeanFK506MulticentreLiverStudyGroup.Lancet,1994,344(8920),423-428.

Reactionmixtureswithpurifiedenzymecontains100nMcalcineurin,100nMcalmodulin,and5μM ³²P-labeledphosphopeptide,in60μL(totalvolume)ofassaybuffercontaining20mMTris(pH8),100mMNaCl,6mMMgCl₂,0.5mMdithiothreitol,0.1mgofbovineserumalbuminpermL,andeither0.1mMCaCl₂or5mMEGTA.Reactionmixtureswithcelllysatescontains20μLofundilutedlysate,5μM ³²P-labeledphosphopeptide,and40μLofassaybuffer.Reactionmixturescontains50μMpeptide412or413and/or500nMokadaicacid,aspecificinhibitorofphosphatases1and2A;500nMokadaicacidissufficientforinhibitionofCa²⁺-independentphosphatases,whereashigherconcentrationspartiallyinhibitCa²⁺-dependentactivityaswell.After15minat30°C,reactionsareterminatedbytheadditionof0.5mLof100mMpotassiumphosphatebuffer(pH7.0)containing5%trichloroaceticacid.FreeinorganicphosphateisisolatedbyDowexcation-exchangechromatographyandquantitatedbyscintillationcountingasdescribed.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CyclosporinAisdissolvedinethanol.

Immunosuppressiveagentsaredissolvedinethanolatconcentrations1000-foldmorethantheconcentrationdesiredforcelltreatments.Cells(10⁶)aresUSPendedin1mLofcompletemediuminmicrocentrifugetubes;1μLofethanoloroftheethanolicsolutionofCyclosporinAisadded,andthecellsareincubatedat37°Cfor1hr.Cellsarewashedtwicewith1mLofPBSoniceandlysedin50μLofhypotonicbuffercontaining50mMTris(pH7.5);0.1mMEGTA;1mMEDTA;0.5mMdithiothreitol;and50μgofphenylmethylsulfonylfluoride,50μgofsoybeantrypsininhibitor,5μgofleupeptin,and5μgofaprotininpermL.Lysatesaresubjectedtothreecyclesoffreezinginliquidnitrogenfollowedbythawingat30°Candthenarecentrifugedat4°Cfor10minat12,000×g.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CyclosporinAissuspendedin0.5%solutionoftragacanth.

Ratsareimmunizedonday0i.p.with05mLandmicei.v.with02mLofa10%suspensionofwashedsheeperythrocytes(SE).Toelicitasecondaryresponse,miceareboosted8-11weeksaftertheprimaryimmunizationwithani.v.injectionof0-2mLof025%washedSE(10⁷cells).Forprolongedtreatmenttheanimalsreceiveontheaverage45mg/kgcyclosporinAdailyinthefoodduring13weeks.Theseratsareimmunized5daysbeforekilling.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].HandschumacherRE,etal.Cyclophilin:aspecificcytosolicbindingproteinforcyclosporinA.Science.1984Nov2;226(4674):544-7.

  [2].LiuJ,etal.Calcineurinisacommontargetofcyclophilin-cyclosporinAandFKBP-FK506complexes.Cell.1991Aug23;66(4):807-15.

  [3].FrumanDA,etal.CalcineurinphosphataseactivityinTlymphocytesisinhibitedbyFK506andcyclosporinA.ProcNatlAcadSciUSA.1992May1;89(9):3686-90.

  [4].FlanaganWM,etal.NuclearassociationofaT-celltranscriptionfactorblockedbyFK-506andcyclosporinA.Nature.1991Aug29;352(6338):803-7.

  [5].NicolliA,etal.Interactionsofcyclophilinwiththemitochondrialinnermembraneandregulationofthepermeabilitytransitionpore,andcyclosporinA-sensitivechannel.JBiolChem.1996Jan26;271(4):2185-92.

  [6].BorelJF,etal.Effectsofthenewanti-lymphocyticpeptidecyclosporinAinanimals.Immunology.1977Jun;32(6):1017-25.

  [7].Williams,R,etal.Randomisedtrialcomparingtacrolimus(FK506)andcyclosporininpreventionofliverallograftrejection.EuropeanFK506MulticentreLiverStudyGroup.Lancet,1994,344(8920),423-428.

1202.61

C₆₂H₁₁₁N₁₁O₁₂

59865-13-3

RoomtemperatureincontinentalUS;mayvaryelsewhere

10mMinDMSO

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:>98.0%

SelectBatch:HY-B0579-11724

DataSheet(124KB)SDS(405KB)

COA(94KB)HNMR(332KB)

HandlingInstructions(1252KB)

• [1].HandschumacherRE,etal.Cyclophilin:aspecificcytosolicbindingproteinforcyclosporinA.Science.1984Nov2;226(4674):544-7.

  [2].LiuJ,etal.Calcineurinisacommontargetofcyclophilin-cyclosporinAandFKBP-FK506complexes.Cell.1991Aug23;66(4):807-15.

  [3].FrumanDA,etal.CalcineurinphosphataseactivityinTlymphocytesisinhibitedbyFK506andcyclosporinA.ProcNatlAcadSciUSA.1992May1;89(9):3686-90.

  [4].FlanaganWM,etal.NuclearassociationofaT-celltranscriptionfactorblockedbyFK-506andcyclosporinA.Nature.1991Aug29;352(6338):803-7.

  [5].NicolliA,etal.Interactionsofcyclophilinwiththemitochondrialinnermembraneandregulationofthepermeabilitytransitionpore,andcyclosporinA-sensitivechannel.JBiolChem.1996Jan26;271(4):2185-92.

  [6].BorelJF,etal.Effectsofthenewanti-lymphocyticpeptidecyclosporinAinanimals.Immunology.1977Jun;32(6):1017-25.

  [7].Williams,R,etal.Randomisedtrialcomparingtacrolimus(FK506)andcyclosporininpreventionofliverallograftrejection.EuropeanFK506MulticentreLiverStudyGroup.Lancet,1994,344(8920),423-428.

品牌介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-Tropanylindole-3-carboxylate;lαH，5Αh-Tropan-3α-ylindole-3-carboxylate中文名称:托烷司琼中文同义词:托普西隆;托普西龙;曲匹西龙;托烷司琼;Β-托烷司琼;CS-348;Β-内托烷司琼;吲哚-3-甲酰氯;Β-托烷司琼(光学异构体);Β-托烷司琼,托烷司琼异构体CBNumber:CB3236404分子式:C17H20N2O2分子量:284.35MOLFile:89565-68-4.mol化学性质安全信息用途供应商112化学性质安全信息用途供应商112托烷司琼化学性质熔点:201-202°C沸点:448.5±35.0°C(Predicted)密度:1.26储存条件:2-8°C溶解度:H2O:soluble形态:solid酸度系数(pKa):15.38±0.30(Predicted)颜色:whiteCAS数据库:Chemicalbook89565-68-4(CASDataBaseReference)安全信息WGKGermany:3托烷司琼化学药品说明书托烷司琼|药物应用信息托烷司琼性质、用途与生产工艺临床评价Sorbe等报道本品对含顺铂(剂量50～89mg/m2)化疗方案引起的急性呕吐完全控制率为63%。58例恶性肿瘤化疗所致恶心、呕吐者，应用托烷司琼或昂丹司琼8mg分别在同一病人前后2个化疗周期的第1d给药前30min静脉注射，并用地塞米松10mg静脉滴注。结果两药控制急性及迟发性恶心、呕吐的疗效基本相似，均可达81%～100%。本品对强致吐化疗药物顺铂的止吐疗效突出。药物相关作用饮食可略为延长本品的吸收。本品与利福平、苯巴比妥等肝酶诱导药同时使用，可加快代谢，故快代谢型者需增加剂量，慢者则不必。西咪替丁等肝酶抑制药对本品血药浓度无明显影响。适应症托烷司琼临床用于预防和治疗癌症化疗引起的恶心和呕吐。化学性质结晶，熔点201-202℃(二氯甲烷-乙酸乙酯)。单盐酸托烷司琼(TropisetronMonohydroehloride)：C17H20N2O2?HCI。[105826-92-4]。熔点283-285℃(分解)。用途有高效性和选择性的5-HT3受体拮抗剂。用于化疗所致的呕吐。用途为5-羟色胺拮抗药生产方法托品醇(I)和酰氯(Ⅱ)反应，可得托烷司琼。托烷司琼上下游产品信息上游原料托品醇下游产品

公司介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-

品牌分类

黄酮类化合物 抑制性抗体 苯丙素类 酸和醛 醌类 肽 其他 酚类 萜类和糖苷类

类固醇 生物碱 糖类和糖苷类 染料试剂 生化分析试剂

显示分类

联络我们

服务热线：4000-520-616

（限工作日9:00-18:00）

QQ ：1570468124

手机：18915418616

官网：http://www.medchemexpress.com/

快速导航：

公司介绍

产品中心

新闻动态

在线咨询

联系我们

公司介绍

产品中心

新闻动态

在线咨询

联系我们

总部地址：

江苏省苏州市工业园区星湖街218号 苏州生物医药产业园一期（生物纳米园）A4-216(邮编：215125)

工作时间：周一至周五9:00~18:00

技术支持：

Email：info@ebiomall.com

短信：18915418616

服务热线：

4000-520-616（全国）

☏  0512-67156496（苏州）

版权信息：

©  2015-2022 苏州蚂蚁淘生物科技有限公司 版权所有 中国

网站备案：

苏ICP备17049038号-1

苏公网安备 32059002001627号

友情链接：

联系QQ:764052152

medix官网 medkoo代购 megazyme正品 microspheres清关 midlandsci采购 minerva报价 molecular molinnov moltox mpbio RevMAb中国 ​​polysciences药物筛选 enogene公司 Viskase Corporation apolloAPI华东代理 美国Novus Immunology Consultan 蚂蚁淘 广东海达仪器制造有限公司

免责声明：

本站有部分内容来自互联网，如无意中侵犯了某个媒体 、公司 、企业或个人等的知识产权，请来电或致函告之，
本网站将在规定时间内给予删除等相关处理。

扫描二维码关注官方微信

获取最新促销及产品信息