GW-1100isaselectiveGPR40antagonistwithapIC₅₀of6.9.GW1100actsasaGPR40inverseagonist.

pIC50:6.9(GPR40)^[1]

GW-1100(GW1100)dosedependentlyinhibitsGPR40-mediatedCa²⁺elevationsstimulatedbyGW9508andlinoleicacid(pIC₅₀valuesof5.99±0.03and5.99±0.06,respectively).GW-1100ataconcentrationof1μMproducesasignificantrightwardshiftintheconcentration-responsecurvetoGW9508(pEC₅₀=7.17±0.08intheabsenceandpEC₅₀=6.79±0.09inthepresenceof1μMGW-1100;P<0.05; n="3)." at="" concentrations="" of="" gw-1100="" of="" 3="" μm="" and="" higher="" a="" significant="" decrease="" in="" the="" maximal="" response="" is="" observed="" with="" a="" continuing="" rightward="" shift="" in="" the="">₅₀response^[2].GW-1100(GW1100)reducesFFAR1ligand-inducedintracellularcalciuminCHO-K1/bFFAR1cellsandneutrophils.CHO-K1/bFFAR1cellsareincubatedfor15minwith10μMGW1100orvehicle(0.1%DMSO)andthenstimulatedwithvehicle,oleicacid,linoleicacidorGW9508.GW-1100significantlyreducestheincreaseinintracellularcalciuminducedby300μMoleicacid(AUC_(60-150s),p<0.05), 100="" μm="" linoleic="" acid="">_(60-150s),p<0.05) and="" 10="" μm="" gw9508="">_(60-150s),p<>^[3].

TheintracerebroventricularinjectionofDHA(50µg)andGW9508(1.0µg),aGPR40-selectiveagonist,significantlyreducesmechanicalallodyniaandthermalhyperalgesiaatday7,butnotatday1,afterCFAinjection.TheseeffectsareinhibitedbyintracerebroventricularpretreatmentwithGW-1100(10µg),aGPR40antagonist^[4].

• [1].StoddartLA,etal.UncoveringthepharmacologyoftheGprotein-coupledreceptorGPR40:highapparentconstitutiveactivityinguanosine5"-O-(3-[35S]thio)triphosphatebindingstudiesreflectsbindingofanendogenousagonist.MolPharmacol.2007Apr;71(

  [2].BriscoeCP,etal.PharmacologicalregulationofinsulinsecretioninMIN6cellsthroughthefattyacidreceptorGPR40:identificationofagonistandantagonistsmallmolecules.BrJPharmacol.2006Jul;148(5):619-28.

  [3].ManosalvaC,etal.Cloning,identificationandfunctionalcharacterizationofbovinefreefattyacidreceptor-1(FFAR1/GPR40)inneutrophils.PLoSOne.2015Mar19;10(3):e0119715.

  [4].NakamotoK,etal.HypothalamicGPR40signalingactivatedbyfreelongchainfattyacidssuppressesCFA-inducedinflammatorychronicpain.PLoSOne.2013Dec12;8(12):e81563.

GW-1100(GW1100)ispreparedinDMSOandstored,andthendilutedwithappropriatemedium(DMSO0.1%)beforeuse^[3].

CHO-K1/bFFAR1orCHO-K1/pCDNA3.1cells(2×10⁶cells/2mL)areloadedwith2.5μMFura-2AMfluorescentindicatordyeinrecordingbuffer(10mMHEPES,140mMNaCl,2mMCaCl₂,21mMMgCl₂,25mMKCl,10mMglucose,pH7.4)for30min,washedthreetimeswithrecordingbuffer,andreturnedtotheincubatorfor10min.Cellsareincubatedwithdifferentconcentrationsofpropionicacid(1,10and30mM),oleicacid(0-500μM),linoleicacid(0-200μM),GW9508(0-100μM),ionomycin(2μM),thapsigargin(2μM)orvehicle(0.1%DMSO).Thefattyacidconcentrationsusedinallexperimentsareintherangeofconcentrationsofhealthyandperipartumcows.Inanothersetofexperiments,cellsareincubatedwitheither10μMGW-1100for15min,2μMU73122for3minorvehicle(0.1%DMSO)for15minandthenstimulatedwitheither300μMoleicacid,100μMlinoleicacidor10μMGW9508.Cellularfluorescence(Ca²⁺)ismeasuredat509nmemissionwith340/380nmdualwavelengthexcitationusingaLS55spectrofluorimeter.Cuvettetemperaturesaremaintainedat37°Cwithconstantstirring^[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

GW-1100(GW1100)ispreparedinDMSOanddilutedwithsalineorPBS^[4].

Mice^[4]
MaleddYmice(age,4weeks)arehousedincagesat23-24°Cwitha12-hlight-darkcycle(lightsfrom8amto8pm)andfoodandwateradlibitum.DHA(50µg/mouse),theselectiveGPR40-agonistGW9508(1.0-25µg/mouse)andtheGPR40antagonistGW1100(1-10µg/mouse)aredissolvedin1%DMSOandthesolutionisdilutedwithsalinebeforevonFreytesting(1%DMSOfinalconcentration).ThedosesofGW9508arechosenbaseduponourpreviouspublication,whereasGW-1100isselectedonthebasisofpreviousreportsandourpreliminaryexperiments.Underanon-anesthetizedstate,DHAandGW9508areadministeredviatheintracerebroventricular(i.c.v.)route10minbeforeCFAinjection,andGW1100isadministeredviathei.c.v.route10minbeforeGW9508injection.Flavopiridol(5and15nmol/mouse),acyclin-dependentkinaseinhibitor,isadministeredbyi.c.v.injectionintotheleftlateralventricleofthemicetwiceaday(at9:00and19:00)afterCFAtreatment.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].StoddartLA,etal.UncoveringthepharmacologyoftheGprotein-coupledreceptorGPR40:highapparentconstitutiveactivityinguanosine5"-O-(3-[35S]thio)triphosphatebindingstudiesreflectsbindingofanendogenousagonist.MolPharmacol.2007Apr;71(

  [2].BriscoeCP,etal.PharmacologicalregulationofinsulinsecretioninMIN6cellsthroughthefattyacidreceptorGPR40:identificationofagonistandantagonistsmallmolecules.BrJPharmacol.2006Jul;148(5):619-28.

  [3].ManosalvaC,etal.Cloning,identificationandfunctionalcharacterizationofbovinefreefattyacidreceptor-1(FFAR1/GPR40)inneutrophils.PLoSOne.2015Mar19;10(3):e0119715.

  [4].NakamotoK,etal.HypothalamicGPR40signalingactivatedbyfreelongchainfattyacidssuppressesCFA-inducedinflammatorychronicpain.PLoSOne.2013Dec12;8(12):e81563.

520.58

C₂₇H₂₅FN₄O₄S

306974-70-9

RoomtemperatureincontinentalUS;mayvaryelsewhere

10mMinDMSO

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

Purity:95.13%

SelectBatch:HY-50691-04737

DataSheet(123KB)SDS(120KB)

COA(94KB)HNMR(204KB)LCMS(170KB)

HandlingInstructions(1252KB)

• [1].StoddartLA,etal.UncoveringthepharmacologyoftheGprotein-coupledreceptorGPR40:highapparentconstitutiveactivityinguanosine5"-O-(3-[35S]thio)triphosphatebindingstudiesreflectsbindingofanendogenousagonist.MolPharmacol.2007Apr;71(

  [2].BriscoeCP,etal.PharmacologicalregulationofinsulinsecretioninMIN6cellsthroughthefattyacidreceptorGPR40:identificationofagonistandantagonistsmallmolecules.BrJPharmacol.2006Jul;148(5):619-28.

  [3].ManosalvaC,etal.Cloning,identificationandfunctionalcharacterizationofbovinefreefattyacidreceptor-1(FFAR1/GPR40)inneutrophils.PLoSOne.2015Mar19;10(3):e0119715.

  [4].NakamotoK,etal.HypothalamicGPR40signalingactivatedbyfreelongchainfattyacidssuppressesCFA-inducedinflammatorychronicpain.PLoSOne.2013Dec12;8(12):e81563.

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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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