H-89(dihydrochloride)isapotentinhibitorofcyclicAMP-dependentproteinkinase(proteinkinaseA)withIC₅₀of48nMandhasweakinhibitiononPKG,PKC,CaseinKinase,andotherskinases.

IC50:48nM(proteinkinaseA)

H-89inhibitsproteinkinaseA,incompetitivefashionagainstATP.H-89causesadose-dependentinhibitionoftheforskolin-inducedproteinphosphorylation,withnodecreaseinintracellularcyclicAMPlevelsinPC12Dcells.H-89significantlyinhibitstheforskolin-inducedneuriteoutgrowthfromPC12Dcells.H-89(30μM)inhibitssignificantlycAMP-dependenthistoneIIbphosphorylationactivityinPC12Dcelllysates^[1].H-89(1-2μM)significantlyslowsthereprimingrateinratskinnedfibres,mostlikelyduetoitdeleteriouslyaffectingtheT-systempotential.H-89(10-100μM)inhibitsnetCa²⁺uptakebytheSRandaffectestheCa²⁺-sensitivityofthecontractileapparatusinratskinnedfibres^[2].

H-89(0.2mg/100g,i.p.)significantlyincreasesseizurelatencyandthresholdinPTZ-treatedanimals.H-89(0.05,0.2mg/100g,i.p.)preventstheepileptogenicactivityofbucladesine(300nM)withsignificantincreaseofseizurelatencyandseizurethreshold^[3].

• [1].ChijiwaT,etal.Inhibitionofforskolin-inducedneuriteoutgrowthandproteinphosphorylationbyanewlysynthesizedselectiveinhibitorofcyclicAMP-dependentproteinkinase,N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide(H-89),ofPC12D

  [2].BlazevR,etal.EffectsofthePKAinhibitorH-89onexcitation-contractioncouplinginskinnedandintactskeletalmusclefibres.JMuscleResCellMotil.2001;22(3):277-86.

  [3].Hosseini-ZareMS,etal.EffectsofpentoxifyllineandH-89onepileptogenicactivityofbucladesineinpentylenetetrazol-treatedmice.EurJPharmacol.2011Nov30;670(2-3):464-70.

Kinaseactivitiesareassayedat30°Cfor2-5minbymeasuringthetransferof³²Pfrom[γ-³²P]ATPtosubstrates.Thereactionisterminatedbyadding1mLof20%trichloroaceticacid,followingtheadditionof100μgofbovineserumalbuminasacarrierprotein.Thesampleiscentrifugedat3000rpmfor10min,thepelletisresUSPendedin5%trichloroaceticacidsolution,thefinalpelletisdissolvedin1mLof1NNaOHandtherADIoactivityismeasuredinaliquidscintillationcounter.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

After48hinculture,PCl2Dcellsareculturedintestmediumcontaining30μMH-89for1handthenexposedtofreshmediumthatcontainedboth10μMforskolinand30μMH-89.Cellsarescrapedoffwitharubberpolicemanandsonicatedinthepresenceof0.5mLof6%trichloroaceticacid.Toextracttrichloroaceticacid,2mLofpetroleumetherisadded,thepreparationmixedandcentrifugedat3000rpmfor10min.Afteraspirationoftheupperlayer,theresiduesamplesolutionisusedfordetermination.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

H-89isdissolvedinDMSOanddistilledwater(10%).

Malealbinomiceweighing20-25gareobtained.Pentoxifylline(25,50,100mg/kg),bucladesine(50,100,300nM/mouse)andH-89(0.05,0.1,0.2mg/100g)areadministeredintraperitoneally(i.p.)30minbeforeintravenous(i.v.)infusionofPTZ.Incombinationgroups,thefirstandsecondcomponentsareinjected45and30minbeforePTZinfusion.Inallgroups,therespectivecontrolanimalsreceiveanappropriatevolumeofvehicle.Forthei.v.infusion,theneedleisinsertedintothelateraltailvein,fixedtothetailveinbyanarrowpieceofadhesivetape,andtheanimalisallowedtomovefreely.PTZsolutionisinfusedataconcentrationrateof1mL/min.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].ChijiwaT,etal.Inhibitionofforskolin-inducedneuriteoutgrowthandproteinphosphorylationbyanewlysynthesizedselectiveinhibitorofcyclicAMP-dependentproteinkinase,N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide(H-89),ofPC12D

  [2].BlazevR,etal.EffectsofthePKAinhibitorH-89onexcitation-contractioncouplinginskinnedandintactskeletalmusclefibres.JMuscleResCellMotil.2001;22(3):277-86.

  [3].Hosseini-ZareMS,etal.EffectsofpentoxifyllineandH-89onepileptogenicactivityofbucladesineinpentylenetetrazol-treatedmice.EurJPharmacol.2011Nov30;670(2-3):464-70.

519.28

C₂₀H₂₂BrCl₂N₃O₂S

130964-39-5

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:≥50mg/mL

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

Purity:98.94%

SelectBatch:HY-15979A-26644HY-15979A-13164HY-15979A-26506

DataSheet(122KB)SDS(120KB)

COA(94KB)HNMR(246KB)RP-HPLC(110KB)LCMS(109KB)

HandlingInstructions(1252KB)

• [1].ChijiwaT,etal.Inhibitionofforskolin-inducedneuriteoutgrowthandproteinphosphorylationbyanewlysynthesizedselectiveinhibitorofcyclicAMP-dependentproteinkinase,N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide(H-89),ofPC12D

  [2].BlazevR,etal.EffectsofthePKAinhibitorH-89onexcitation-contractioncouplinginskinnedandintactskeletalmusclefibres.JMuscleResCellMotil.2001;22(3):277-86.

  [3].Hosseini-ZareMS,etal.EffectsofpentoxifyllineandH-89onepileptogenicactivityofbucladesineinpentylenetetrazol-treatedmice.EurJPharmacol.2011Nov30;670(2-3):464-70.

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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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