TacrolimusbindstoFK506bindingprotein(FKBP).Thiscomplexinhibitscalcineurinphosphatase(PP2B).TacrolimusisamTOR-independentautophagyinducer.

PP2B(calcineurinphosphatase)^[1]
Autophagyinducer^[2]

Tacrolimus(FK506)inhibitscalcium-dependentevents,suchasIL-2genetranscription,NOsynthaseactivation,celldegranulation,andapoptosis.TacrolimusalsopotentiatestheactionsofglucocorticoidsandprogesteronebybindingtoFKBPscontainedwithinthehormonereceptorcomplex,preventingdegradation.TheagentmayenhanceexpressionoftheTGFβ-1geneinafashionanalogoustothatdemonstratedforCsA.TcellproliferationinresponsetoligationoftheTcellreceptorisinhibitedbyTacrolimus^[1].Tacrolimus(FK506)isapowerfulimmunosuppressivedrugwidelyusedtopreventorganrejectionaftertransplantation.Tacrolimusinhibitothercalcineurin-dependenttranscriptionfactorsincludingtheubiquitouslyexpressedcAMPresponseelement-bindingprotein(CREB).TacrolimusinhibitCREBtranscriptionalactivityatthecoactivatorlevel.Thedepolarization-inducedtranscriptionalactivityoftheCBPC-terminusisenhancedbyoverexpressionofcalcineurinandisinhibitedbyTacrolimusinaconcentration-dependentmannerwithIC₅₀of1nMconsistentwithIC₅₀forinhibitionofcalcineurin^[3].

Inthepleurisyinducedbycarrageenan,Tacrolimus(1mg/kg,i.p.)andDexamethasone(0.5mg/kg,i.p.)admiNISTered0.5hbeforecausesasignificantdecreaseinleukocytes,neutrophilsandexudation(P<0.01). under="" the="" same="" conditions,="" tacrolimus="" and="" dexamethasone="" do="" not="" modify="" the="" blood"s="" white="" or="" red="" cells="" (p="">0.05).Tacrolimusshowsalonglastingantiinflammatoryeffect,inhibitingleukocytesandneutrophilsforupto24h(P<0.01), whereas="" the="" inhibition="" of="" exudation="" is="" less="" marked="" (up="" to="" 2="" h)=""><0.01). these="" drugs="" caused="" a="" marked="" reduction="" in="" mpo="" activity,="" as="" well="" as="" il-1β="" and="" tnfα="" levels=""><0.01), but="" only="" tacrolimus="" inhibits="" ada="" activity=""><0.01). tacrolimus="" significantly="" inhibits="" cell="" migration="" induces="" by="" either="" bradykinin,="" histamine="" or="" substance="" p=""><>^[4].

• [1].ThomsonAW,etal.ModeofactionofTacrolimus(FK506):molecularandcellularmechanisms.TherDrugMonit.1995Dec;17(6):584-91.

  [2].VogelKR,etal.mTORinhibitorsrescueprematurelethalityandattenuatedysregulationofGABAergic/glutamatergictranscriptioninmurinesuccinatesemialdehydedehydrogenasedeficiency(SSADHD),adisorderofGABAmetabolism.JInheritMetabDis.2016Nov;39(6):877-886.

  [3].OetjenE,etal.TheimmunosuppressivedrugscyclosporinAandtacrolimusinhibitmembranedepolarization-inducedCREBtranscriptionalactivityatthecoactivatorlevel.BrJPharmacol.2005Apr;144(7):982-93.

  [4].PereiraR,etal.AntiinflammatoryeffectsofTacrolimusinamousemodelofpleurisy.TransplImmunol.2006Aug;16(2):105-11.

Tacrolimus(FK506)isdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse^[3].

Thepancreaticisletβ-celllineHITisgrowninRPMI1640supplementedwith10%fetalcalfserum,5%horseserum,100U/mLPenicillin,and100μg/mLStreptomycin.HITcellsaretransientlytransfectedbytheDEAE-dextranmethodwith2μgofindicatorplasmidper6-cmdishand2μgofexpressionvectorper6-cmdish,unlessstatedotherwise.Roussarcomavirus-chloramphenicolacetyltransferase(0.5μgper6-cmdish)orcytomegalovirusgreenfluorescentproteinexpressionvectors(1μgper6-cmdish)areaddedassecondreporterstocontrolfortransfectionefficiency.CotransfectionsarecarriedoutwithaconstantDNAconcentration,whichismaintainedbyaddingtheemptyvector.CellsarestimulatedwithhighKCl(finalconcentration45mM)orcAMP(forskolin10μM)6hbeforeharvest,cyclosporinAorTacrolimusareadded1hbeforestimulation.Cellextractsareprepared48haftertransfection.Thechloramphenicolacetyltransferaseassayandtheluciferaseassayareperformed.FluorescenceofthegreenfluorescentproteinismeasuredinaPackardFluoroCountwithexcitationwavelengthat485nmandemissionwavelengthat530nm^[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Tacrolimus(FK506)isdissolvedinsterilesaline(NaCl0.9%)(Mice)^[4].

Mice^[4]
Swissmice,weighing18-22g,arerandomlyallocatedintwelvegroups:(1)Control-treatedwithsterilesaline(NaCl,0.9%,intrapleuralroute),(2)Cg(1%,ipl.),(3)Cg(1%,ipl.)plusTacrolimus(0.5-1.5mg/kg,i.p.),(4)Cg(1%,ipl.)plusdexametahasone(0.5mg/kg,i.p.),(5)BK(10nmol,ipl.),(6)BK(10nmol,ipl.)plusTacrolimus(1.0mg/kg,i.p.),(7)Bradykinin(10nmol,ipl.)plusDexamethasone(0.5mg/kg,i.p.),(8)Histamine(1μg,ipl.),Histamine(1μg,ipl.)plusTacrolimus(1.0mg/kg,i.p.),(9)Histamine(1μg,ipl.)plusDexamethasone(0.5mg/kg,i.p.),(10)SP(20nmol,ipl.,(11),SP(20nmol,ipl.)plusTacrolimus(1.0mg/kg,i.p.),and(12)SP(20nmol,ipl.)plusDexamethasone(0.5mg/kg,i.p.).TacrolimusandDexamethasoneareadministered0.5hpriortopleurisyinduction.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].ThomsonAW,etal.ModeofactionofTacrolimus(FK506):molecularandcellularmechanisms.TherDrugMonit.1995Dec;17(6):584-91.

  [2].VogelKR,etal.mTORinhibitorsrescueprematurelethalityandattenuatedysregulationofGABAergic/glutamatergictranscriptioninmurinesuccinatesemialdehydedehydrogenasedeficiency(SSADHD),adisorderofGABAmetabolism.JInheritMetabDis.2016Nov;39(6):877-886.

  [3].OetjenE,etal.TheimmunosuppressivedrugscyclosporinAandtacrolimusinhibitmembranedepolarization-inducedCREBtranscriptionalactivityatthecoactivatorlevel.BrJPharmacol.2005Apr;144(7):982-93.

  [4].PereiraR,etal.AntiinflammatoryeffectsofTacrolimusinamousemodelofpleurisy.TransplImmunol.2006Aug;16(2):105-11.

804.02

C₄₄H₆₉NO₁₂

104987-11-3

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:≥28mg/mL

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

Purity:98.46%

SelectBatch:HY-13756-22811HY-13756-22451HY-13756-26336HY-13756-21691HY-13756-22712HY-13756-18778HY-13756-19712HY-13756-13591

DataSheet(127KB)SDS(277KB)

COA(96KB)HNMR(394KB)LCMS(141KB)

HandlingInstructions(1252KB)

• [1].ThomsonAW,etal.ModeofactionofTacrolimus(FK506):molecularandcellularmechanisms.TherDrugMonit.1995Dec;17(6):584-91.

  [2].VogelKR,etal.mTORinhibitorsrescueprematurelethalityandattenuatedysregulationofGABAergic/glutamatergictranscriptioninmurinesuccinatesemialdehydedehydrogenasedeficiency(SSADHD),adisorderofGABAmetabolism.JInheritMetabDis.2016Nov;39(6):877-886.

  [3].OetjenE,etal.TheimmunosuppressivedrugscyclosporinAandtacrolimusinhibitmembranedepolarization-inducedCREBtranscriptionalactivityatthecoactivatorlevel.BrJPharmacol.2005Apr;144(7):982-93.

  [4].PereiraR,etal.AntiinflammatoryeffectsofTacrolimusinamousemodelofpleurisy.TransplImmunol.2006Aug;16(2):105-11.

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-

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