U-73122isaninhibitorofphospholipaseC(PLC),phospholipaseA2,and5-LO(5-lipoxygenase). 

U-73122potentlyinhibitsreceptor-coupledactivationofPLCinmembranesisolatedfromPMNs^[1].U-73122inhibitsN-formyl-methionyl-leucyl-phenylalanine-inducedaggregationofhumanpolymorphonuclearneutrophils(PMN)andtheassociatedproductionofIP₃anddiacyglycerol^[2].U-73122markedlyinhibitsinositolphosphatereleaseelicitedbyeitheroxotremorine-Morguanosine-5"-O-(3-thiotriphosphate)thanthatinducedbyaddedCa²⁺indigitonin-permeABIlizedcells^[3].

U73122significantlyattenuatesTNF-αmRNAexpression,hasnoeffectonshamanimals,butsignificantlyincreasesheartworkandrateofcontractionandrelaxationwithoutaffectingheartrateinendotoxemicmice^[4].U73122(400nM/µL)significantlyreducestotallordosisdurations,comparedtovehicleinfusionstotheVTA,ofoestrADIolandprogesterone-primedhamsters.VTAinfusionsofU73122donotaltermotorbehaviourofhamstersintheactivitymonitor,butthereisasignificanteffectofmuscimoltodecreasetotalnumberofbeambreakscomparedtohamstersadmiNISTeredSKF38393^[5].

• [1].SmithRJ,etal.Receptor-coupledsignaltransductioninhumanpolymorphonuclearneutrophils:effectsofanovelinhibitorofphospholipaseC-dependentprocessesoncellresponsiveness.JPharmacolExpTher.1990May;253(2):688-97.

  [2].BleasdaleJE,etal.Selectiveinhibitionofreceptor-coupledphospholipaseC-dependentprocessesinhumanplateletsandpolymorphonuclearneutrophils.JPharmacolExpTher.1990Nov;255(2):756-68.

  [3].ThompsonAK,etal.TheaminosteroidU-73122inhibitsmuscarinicreceptorsequestrationandphosphoinositidehydrolysisinSK-N-SHneuroblastomacells.AroleforGpinreceptorcompartmentation.JBiolChem.1991Dec15;266(35):23856-62.

  [4].PengT,etal.DisruptionofphospholipaseCgamma1signallingattenuatescardiactumornecrosisfactor-alphaexpressionandimprovesmyocardialfunctionduringendotoxemia.CardiovascRes.2008Apr1;78(1):90-7.Epub2007Dec12.

  [5].FryeCA,etal.Intheventraltegmentalarea,themembrane-mediatedactionsofprogestinsforlordosisofhormone-primedhamstersinvolvephospholipaseCandproteinkinaseC.JNeuroendocrinol.2007Sep;19(9):717-24.

PMNs(4×10⁷/4mL)areincubatedwithU-73122accordingtoprotocols.Thereactionsarestoppedwithcoldcalcium-freePBS.Thecellsarecentrifugedat750×g(4°C)andresUSPendedin1mLofTritonX-100-freeextractionbuffer(50mMTris,pH7.5,50mMfimercaptoethanol,2mMEGTA,1mMphenylmethylsulfonylfluorideand4μg/mLofleupeptin,soybeantrypsininhibitorandaprotinin),andthensonicatedfor10-and5-secconsecutiveburstsat20%output.Thelysatesarecentrifugedat240×g(4°C)for20mminaTL-100ultracentrifugewiththesupernatantdesignatedasthecytosolfraction.Thepelletisresuspendedin1%Triton-containingextractionbuffer,sonicated,shakenfor30mmat4°Candcentrifuged(240×gfor20mmat4°C).Thesupernatantconstitutestheextractableparticulatefraction,andthepelletissonicatedinextractionbufferwithTritonandconstitutedthenonextractableparticulatefraction.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

U-73122isdissolvedinDMSO.

Agonist-inducedproductionofIP₃inPMNismeasuredbyuseofthecompetitiveradiobindingassy.PMN(2x10⁶-10⁷)in0.2mLofphosphate-bufferedsaline,pH7.4[NaC1(138mM),Na₂HPO₄(8.1mM),KH₂PO₄(1.5mM),KCI(2.7mM),CaCl₂(1.0mM),MgC1₂(1.0mM)andglucose(0.1%,w/v)]areincubatedinconicalpolypropylenetubesat37°Cinashakingwaterbath.U-73122orU-73343isadded(in1μLofDMSO)3minbeforetheadditionofagonist,FMLP(0.1μM)pluscytochalasinB(5μg/mL).FMLPandcytochalasinBareaddedin1μLeachofDMSOandethanol,respectively.Appropriatevehiclecontrolsareincludedineachexperiment.PMNincubationmixturesarequenchedwiththeadditionof0.07mLofice-coldTCA(20%,w/v)andaportion(0.2mL)oftheTCAextractisprocessedforthemeasurementofIP₃bycompetitiveradiobindingasdescribedaboveforplatelets.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

U-73122isformulatedinsaline.

Hamstersarehormone-primedwith17β-oestradiolath 0andprogesteroneath 45.Ath 48,hamstersarepretestedformotorbehaviour,followedbysexualbehaviourtesting,andbilateralinfusionsofU73122(400nM/µL)orsalinevehicle.Thirtyminutesafterinfusions,hamstersarere-testedforsexualbehaviour(postinhibitorinfusiontest)and,immediatelyaftertesting,infusedbilaterallywithSKF38393(100ng/µL),muscimol(100ng/µL),orsalinevehicle.Thirtyminutesaftertheagonistorvehicleinfusions,lordosisandmotorbehaviourofhamstersisreassessed(postagonistinfusiontest).Allhamstersareassignedtoonepretreatmentcondition,U73122orvehicle,andaretestedonceaweekfor3weeksuntilallinfusionconditions(SKF38393,muscimolorvehicle),arereceived.TheorderinwhichhamstersreceiveSKF38393,muscimolorvehicleinfusionsiscounterbalancedacrossthegroup. MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].SmithRJ,etal.Receptor-coupledsignaltransductioninhumanpolymorphonuclearneutrophils:effectsofanovelinhibitorofphospholipaseC-dependentprocessesoncellresponsiveness.JPharmacolExpTher.1990May;253(2):688-97.

  [2].BleasdaleJE,etal.Selectiveinhibitionofreceptor-coupledphospholipaseC-dependentprocessesinhumanplateletsandpolymorphonuclearneutrophils.JPharmacolExpTher.1990Nov;255(2):756-68.

  [3].ThompsonAK,etal.TheaminosteroidU-73122inhibitsmuscarinicreceptorsequestrationandphosphoinositidehydrolysisinSK-N-SHneuroblastomacells.AroleforGpinreceptorcompartmentation.JBiolChem.1991Dec15;266(35):23856-62.

  [4].PengT,etal.DisruptionofphospholipaseCgamma1signallingattenuatescardiactumornecrosisfactor-alphaexpressionandimprovesmyocardialfunctionduringendotoxemia.CardiovascRes.2008Apr1;78(1):90-7.Epub2007Dec12.

  [5].FryeCA,etal.Intheventraltegmentalarea,themembrane-mediatedactionsofprogestinsforlordosisofhormone-primedhamstersinvolvephospholipaseCandproteinkinaseC.JNeuroendocrinol.2007Sep;19(9):717-24.

464.64

C₂₉H₄₀N₂O₃

112648-68-7

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:<4.8="">

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

Purity:>98.0%

SelectBatch:HY-13419-14812

DataSheet(125KB)SDS(389KB)

COA(94KB)HNMR(459KB)

HandlingInstructions(1252KB)

• [1].SmithRJ,etal.Receptor-coupledsignaltransductioninhumanpolymorphonuclearneutrophils:effectsofanovelinhibitorofphospholipaseC-dependentprocessesoncellresponsiveness.JPharmacolExpTher.1990May;253(2):688-97.

  [2].BleasdaleJE,etal.Selectiveinhibitionofreceptor-coupledphospholipaseC-dependentprocessesinhumanplateletsandpolymorphonuclearneutrophils.JPharmacolExpTher.1990Nov;255(2):756-68.

  [3].ThompsonAK,etal.TheaminosteroidU-73122inhibitsmuscarinicreceptorsequestrationandphosphoinositidehydrolysisinSK-N-SHneuroblastomacells.AroleforGpinreceptorcompartmentation.JBiolChem.1991Dec15;266(35):23856-62.

  [4].PengT,etal.DisruptionofphospholipaseCgamma1signallingattenuatescardiactumornecrosisfactor-alphaexpressionandimprovesmyocardialfunctionduringendotoxemia.CardiovascRes.2008Apr1;78(1):90-7.Epub2007Dec12.

  [5].FryeCA,etal.Intheventraltegmentalarea,themembrane-mediatedactionsofprogestinsforlordosisofhormone-primedhamstersinvolvephospholipaseCandproteinkinaseC.JNeuroendocrinol.2007Sep;19(9):717-24.

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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

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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-

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