GW4064isapotentFXRagonistwithEC₅₀of65nM.

EC50:65nM(FXR)^[1]

TreatmentwithdifferentconcentrationsofGW4064(1,2.5,5,10μM)reducesthelipidaccumulationinthecells.Concordantly,GW4064treatmentsignificantlyrepressesoleicacid-inducedCD36proteinlevelsinadose-dependentmanner.Takentogether,thesedataindicatethatpreventionofhepaticlipidaccumulationislikelyduetoaninhibitionofCd36expressionbylong-termGW4064treatment^[2].

GW4064suppressesweightgaininC57BL/6micefedwitheitherahigh-fatdiet(HFD)orhigh-fat,high-cholesteroldiet.GW4064treatmentofmiceonHFDsignificantlyrepressesdiet-inducedhepaticsteatosisasevidencedbylowertriglycerideandfreefattyacidlevelintheliver.GW4064markedlyreduceslipidtransporterCD36expressionwithoutaffectingexpressionofgenesthataredirectlyinvolvedinlipogenesis.GW4064treatmentattenuateshepaticinflammationwhilehavingnoeffectonwhiteADIposetissue^[2].GW4064(30mg/kg)treatmentresultsinsubstantial,statisticallysignificantreductionsinserumactivitiesofALT,AST,LDH,andALPintheANIT-treatedrats.SerumbileacidlevelsarealsosignificantlyreducedbyGW4064treatment.BilirubinlevelsaredecreasedintheGW4064-treatedrats,butstatisticalsignificanceisnotachieved.Notably,GW4064ismuchmoreeffectiveindecreasingtheseMarkersofliverdamagethanTUDCA,whichreducesonlyLDHlevels^[3].

• [1].AkwABI-AmeyawA,etal.ConformationallyconstrainedfarnesoidXreceptor(FXR)agonists:Naphthoicacid-basedanalogsofGW4064.BioorgMedChemLett,2008,18(15),4339-4343.

  [2].MaY,etal.SyntheticFXRagonistGW4064preventsdiet-inducedhepaticsteatosisandinsulinresistance.PharmRes.2013May;30(5):1447-57.

  [3].LiuY,etal.HepatoprotectionbythefarnesoidXreceptoragonistGW4064inratmodelsofintra-andextrahepaticcholestasis.JClinInvest.2003Dec;112(11):1678-87.

GW4064isdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse^[2].

Mouselivercells(BNLCL.2)aremaintainedinahumidifiedincubatorunder5%CO2at37°CinDulbecco"sModifiedEagle"sMedium(DMEM)supplementedwith10%fetalbovineserum(FBS)and1%Penicillin/Streptomycin.Whencellsaredividedintosix-wellplatesandreach~90%confluence,sub-confluentcellsarewashedthreetimeswithphosphatebufferedsaline(PBS)andreplacedwithserum-freeDMEMsupplementedwith1%fattyacid-freeBSA.Oleicacid(finalconcentration500μM)andGW4064atvariousconcentrationsareaddedandincubatedfor24h.Cellsarethenfixedwith4%formaldehydeforOilRedOstainingorharvestedforproteinandwesternblotanalysis^[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

GW4064isdissolvedinDMSOanddiluted(Mice)^[2].
GW4064ispreparedincornoil(Rat)^[3].

Mice^[2]
Fifteen-week-oldmaleC57BL/6micearefedahigh-fatdietwithorwithoutadditional0.2%CholesterolandreceivedtwiceweeklyinjectionsofGW4064(50mg/kg,intra-peritoneal)orcarriersolution(DMSO)solutionfor6weeks.AnimalsareweighedweeklyandtheirbodycompositionisdeterminedusingEchoMRI-100^TMfromEchoMedicalSystems.
Rat^[3]
Animals.AdultmaleCRL:CD(SD)IGSratsweighing300-350g,areused.Theratsreceiveasingleanalgesicdoseofoxymorphonefollowingsurgery.Twenty-fourhoursafterlaparotomy,groupsofrats(n=6)receiveintraperitonealinjectionsoncedailyfor4days.Bileduct-ligated(BDL)ratsaretreatedwith5mL/kgcornoilasvehicle,30mg/kgGW4064incornoil,or15mg/kgTUDCAincornoil.Sham-operatedanimalsreceived5mL/kgcornoilvehicle.Fourhoursafterthefinaldose,serumandliversarecollectedforanalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].Akwabi-AmeyawA,etal.ConformationallyconstrainedfarnesoidXreceptor(FXR)agonists:Naphthoicacid-basedanalogsofGW4064.BioorgMedChemLett,2008,18(15),4339-4343.

  [2].MaY,etal.SyntheticFXRagonistGW4064preventsdiet-inducedhepaticsteatosisandinsulinresistance.PharmRes.2013May;30(5):1447-57.

  [3].LiuY,etal.HepatoprotectionbythefarnesoidXreceptoragonistGW4064inratmodelsofintra-andextrahepaticcholestasis.JClinInvest.2003Dec;112(11):1678-87.

542.84

C₂₈H₂₂Cl₃NO₄

278779-30-9

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:≥150mg/mL

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

Purity:99.42%

SelectBatch:HY-50108-25346HY-50108-19260

DataSheet(133KB)SDS(252KB)

COA(95KB)HNMR(471KB)LCMS(162KB)

HandlingInstructions(1252KB)

• [1].Akwabi-AmeyawA,etal.ConformationallyconstrainedfarnesoidXreceptor(FXR)agonists:Naphthoicacid-basedanalogsofGW4064.BioorgMedChemLett,2008,18(15),4339-4343.

  [2].MaY,etal.SyntheticFXRagonistGW4064preventsdiet-inducedhepaticsteatosisandinsulinresistance.PharmRes.2013May;30(5):1447-57.

  [3].LiuY,etal.HepatoprotectionbythefarnesoidXreceptoragonistGW4064inratmodelsofintra-andextrahepaticcholestasis.JClinInvest.2003Dec;112(11):1678-87.

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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