Rivaroxabanisahighlypotentandselective,directFactorXa(FXa)inhibitor,achievingastronggaininanti-FXapotency(IC₅₀0.7nM;K_i0.4nM).

IC50:0.7nM(FXa)^[1]
Ki:0.4nM(FXa)^[1]

Rivaroxaban(BAY59-7939)isanoral,directFactorXa(FXa)inhibitorindevelopmentforthepreventionandtreatmentofarterialandvenousthrombosis.RivaroxabancompetitivelyinhibitshumanFXa(K_i0.4nM)with>10000-foldgreaterselectivitythanforotherserineproteases;italsoinhibitsprothrombinaseactivity(IC₅₀2.1nM).RivaroxabaninhibitsendogenousFXamorepotentlyinhumanandrabbitplasma(IC₅₀21nM)thanratplasma(IC₅₀290nM).Itdemonstratesanticoagulanteffectsinhumanplasma,doublingprothrombintime(PT)andactivatespartialthromboplastintimeat0.23and0.69μM,respectively^[2].

Rivaroxaban(BAY59-7939)isapotentandselective,directFXainhibitorwithexcellentinvivoactivityandgoodoralbioavailABIlity^[1].Rivaroxaban(BAY59-7939),admiNISTeredbyi.v.bolusbeforethrombusinduction,reducesthrombusformation(ED₅₀0.1mg/kg),inhibitsFXa,andprolongsPTdosedependently.PTandFXaareaffectedslightlyattheED₅₀(1.8-foldincreaseand32%inhibition,respectively).At0.3mg/kg(doseleADIngtoalmostcompleteinhibitionofthrombusformation),RivaroxabanmoderatelyprolongsPT(3.2±0.5-fold)andinhibitsFXaactivity(65±3%)^[2].

• [1].RoehrigS,etal.Discoveryofthenovelantithromboticagent5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide(BAY59-7939):anoral,directfactorXainhibitor.JMedChem.2005Sep22;48(19)

  [2].PerzbornE,etal.InvitroandinvivostudiesofthenovelantithromboticagentBAY59-7939--anoral,directFactorXainhibitor.JThrombHaemost.2005Mar;3(3):514-21.

TheactivityofRivaroxaban(BAY59-7939)againstpurifiedserineproteasesismeasuredusingchromogenicorfluorogenicsubstratesin96-wellmicrotiterplatesat25°C.TheenzymesareincubatedwithRivaroxabanoritssolvent,DMSO,for10min.Thereactionsareinitiatedbytheadditionofthesubstrate,andthecolororfluorescenceismonitoredcontinuouslyat405nmusingaSpectraRainbowThermoReader,orat630/465nmusingaSPECTRAfluorplus,respectively,for20min.Enzymaticactivityisanalyzedinthefollowingbuffers(finalconcentrations):humanFXa(0.5nM),rabbitFXa(2nM),ratFXa(10nM),orurokinase(4nM)in50mMTris-HClbuffer,pH8.3,150mMNaCl,and0.1%bovineserumalbumin(BSA);PefachromeFXa(50-800μM)orchromozymU(250μM)withthrombin(0.69nM),trypsin(2.2nM),orplasmin(3.2nM)in0.1μMTris-HCl,pH8.0,and20mMCaCl₂;chromozymTH(200μM),chromozymplasmin(500μM),orchromozymtrypsin(500μM)withFXIa(1nM)orAPC(10nM)in50mMphosphatebuffer,pH7.4,150mMNaCl;andS2366(150or500μM)withFVIIa(1nM)andtissuefactor(3nM)in50mMTris-HClbuffer,pH8.0,100mMNaCl,5mMCaCl₂and0.3%BSA,H-D-Phe-Pro-Arg-6-amino-1-naphthalene-benzylsulfon-amideH₂O(100μM)andmeasuredfor3h.TheFIXab/FXassay,comprisingFIXab(8.8nM)andFX(9.5nM)in50mMTris-HClbuffer,pH7.4,100mMNaCl,5mMCaCl₂and0.1%BSA,isstartedbytheadditionofI-1100(50μM),andmeasuredfor60min.Theinhibitoryconstant(K_i)againstFXaiscalculatedaccordingtotheCheng-Prusoffequation(K_i=IC₅₀/1+[S]/K_m),where[S]isthesubstrateconcentration,andK_mistheMichaelis-Mentenconstant.K_misdeterminedfromaLineweaver-Burkplot.TheIC₅₀istheamountofinhibitorrequiredtodiminishtheinitialvelocityofthecontrolby50%^[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Rivaroxaban(BAY59-7939)isdissolvedinpolyethyleneglycol/H2O/glycerol(Rat)^[2].

Rat^[2]
Fasted,maleWistarrats(HsdCpb:WU)areused.RatvenousstasismodelThrombusformationisinducedinanesthetizedrats(n=10perdosegroup),withminormodifications.TheaBDominalvenacavaisexposedandtwoloosesutures(8-10mmapart)areplacedbelowtheleftrenalvenousbranch.Rivaroxabandissolvedinpolyethyleneglycol/H₂O/glycerol(996g/100g/60g),orvehicleisgivenbyintravenous(i.v.)bolusinjectionintoatailvein15minbeforethrombusinduction.Thromboplastin(0.5mg/kg)isinjectedintoafemoralveinand,after15s,theproximalanddistalsuturesaretied.Fifteenminuteslater,theligatedsegmentisremoved,thethrombuswithdrawnandweighed.Bloodsamplesareobtainedbycardiacpunctureimmediatelybeforethrombusremoval.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].RoehrigS,etal.Discoveryofthenovelantithromboticagent5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide(BAY59-7939):anoral,directfactorXainhibitor.JMedChem.2005Sep22;48(19)

  [2].PerzbornE,etal.InvitroandinvivostudiesofthenovelantithromboticagentBAY59-7939--anoral,directFactorXainhibitor.JThrombHaemost.2005Mar;3(3):514-21.

435.88

C₁₉H₁₈ClN₃O₅S

366789-02-8

RoomtemperatureincontinentalUS;mayvaryelsewhere

10mMinDMSO

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

Purity:99.96%

SelectBatch:HY-50903-10671HY-50903-04896HY-50903-03201HY-50903-02770

DataSheet(123KB)SDS(120KB)

COA(93KB)HNMR(232KB)RP-HPLC(195KB)

HandlingInstructions(1252KB)

• [1].RoehrigS,etal.Discoveryofthenovelantithromboticagent5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide(BAY59-7939):anoral,directfactorXainhibitor.JMedChem.2005Sep22;48(19)

  [2].PerzbornE,etal.InvitroandinvivostudiesofthenovelantithromboticagentBAY59-7939--anoral,directFactorXainhibitor.JThrombHaemost.2005Mar;3(3):514-21.

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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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类固醇 生物碱 糖类和糖苷类 染料试剂 生化分析试剂

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