Angiotensin(1-7)inhibitspurifiedcanineangiotensinconvertingenzyme(ACE)activitywithanIC₅₀of0.65μM.

IC50:0.65μM(ACE)^[1]

Angiotensin1-7(Ang1-7)actsasalocalsynergisticmodulatorofkinin-inducedvasodilationbyinhibitingACEandreleasingnitricoxide(NO).Angiotensin(1-7)augmentsthevasodilationinducedbybradykinin(BK)inaconcentration-dependentmannerinringspreconstrictedwiththethromboxaneanalogU46619.TheEC₅₀ofBK(2.45±0.51nMversus0.37±0.08nM)isshiftedleftwardby6.6-foldinthepresenceof2μMconcentrationofAngiotensin(1-7).TheBK-inducedrelaxationresponseisaugmentedbyAngiotensin(1-7)(0.1to2μM)inadose-dependentmanner.Ataconcentrationof2μMAngiotensin(1-7),relaxationtoBKisincreased92%comparedtoBKalone(41±4.4%versus92±2.5%,P<0.01). angiotensin="" (1-7)="" possesses="" novel="" biological="" functions="" that="" are="" distinct="" from="" ang="" ii.="" in="" contrast="" to="" ang="" ii,="" angiotensin="" (1-7)="" is="" not="" a="" dipsogen="" or="" an="" aldosterone="" secretagogue,="" but="" similar="" to="" ang="" ii,="" it="" stimulates="" the="" release="" of="" vasopressin,="" prostaglandins,="" and="" no.="" angiotensin="" (1-7)="" counteracts="" several="" actions="" of="" ang="" ii.="" in="" both="" canine="" and="" porcine="" coronary="" arteries,="" angiotensin="" (1-7)="" causes="" vasodilation,="" while="" ang="" ii="" divergently="" constricts="" the="" coronary="" arteries.="" angiotensin="" (1-7)="" inhibits="" cultured="" vascular="" smooth="" muscle="" cell="" growth,="" whereas="" equal="" molar="" concentration="" of="" ang="" ii="" stimulates="" cell="">^[1].Angiotensin1-7(Ang1-7)abrogatesthemethylglyoxal-modifiedalbumin(MGA)-stimulatedmyofibroblastphenotypebyinhibitingthechronicstimulationoftheTGF-β-ERKpathwayinNRK-52Ecells^[2].

AsevenfolddecreaseintheplasmalevelofAngiotensin1-7(Ang1-7)isdemonstratedindextransulfatesodium(DSS)treatedmicecomparetountreated(UT)groupatday7postcolitisinduction.Ontheotherhand,asignificantincreaseinAng1-7isobservedincolonhomogenatesofDSStreatedmiceatday7(0.09ng/mL)comparetoUTmice(0.04ng/mL)^[3].Theovariectomized(OV)femaleWistar-ratsreceiveestrADIol(500μg/kg/week)orvehiclefortwoweeks.Theanimalsareanesthetized,cannulated,andtheresponsesincludingmeanarterialpressure,renalbloodflow(RBF),andrenalvascularresistanceattheconstantlevelofrenalperfusionpressuretogradedinfusionofAngiotensin1-7(Ang1-7)at0,100and300ng/kg/minaredeterminedinOVandOVestradiol-treated(OVE)rats,treatedwithvehicleorMasRantagoNIST;A779.RBFresponsetoAng1-7infusionincreaseddose-dependentlyinvehicle(P_dose<0.001) and="" a779-treated="">_dose<0.01) animals.="" however,="" when="" masr="" is="" blocked,="" the="" rbf="" response="" to="" ang="" 1-7="" significantly="" increases="" in="" ov="" animals="" compare="" with="" ove="" rats=""><0.05). when="" estradiol="" is="" limited="" by="" ovariectomy,="" a779="" increases="" rbf="" response="" to="" angiotensin="" (1-7)="" administration,="" while="" this="" response="" is="" attenuated="" in="" ove="">^[4].

• [1].LiP,etal.Angiotensin-(1-7)augmentsbradykinin-inducedvasodilationbycompetingwithACEandreleasingnitricoxide.Hypertension.1997Jan;29(1Pt2):394-400.

  [2].AlzayadnehEM,etal.Angiotensin-(1-7)abolishesAGE-inducedcellularhypertrophyandmyofibroblasttransformationviainhibitionofERK1/2.CellSignal.2014Sep19.pii:S0898-6568(14)00314-3.

  [3].KhajahMA,etal.Anti-InflammatoryActionofAngiotensin1-7inExperimentalColitis.PLoSOne.2016Mar10;11(3):e0150861.

  [4].SaberiS,etal.RoleofMasreceptorinrenalbloodflowresponsetoangiotensin-(1-7)inovariectomizedestradioltreatedrats.ResPharmSci.2016Jan-Feb;11(1):65-72.

CompetitionassaysusingpurifiedcanineACEaredeterminedusingafixedconcentrationofthesubstrateHip-His-Leu(1mM)andvaryingtheconcentrationsofthecompetingagents[Lisinopril(0.1to100nM),Angiotensin(1-7)(10nMto10μM),orSar¹,Thr⁸-AngII(10nMto10μM)].Inhibitoryconstants(IC₅₀)aredeterminedfromtherespectivecompetitioncurves.TostudytheeffectofAngiotensin(1-7)onBKmetabolisminintactcoronaryrings,¹²⁵I-[Tyr⁰]-BK(finalconcentrationof1nM)isaddedtothetubescontainingthreeringspreincubatedwith1mLKrebs"bufferandaeratedwith95%O₂and5%CO₂at37°C.Lisinopril(2μM),Angiotensin(1-7)(2μM),orKrebs"bufferascontrolareaddedtotherings10minutesbeforeadditionoftheradiolabeledBK.Aliquotsoftheincubationmediumareremovedat5,10,and20minutesanddilutedwith1%HFBAtoinhibitpeptidaseactivity^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Angiotensin1-7(Ang1-7)ispreparedinsaline^[2].

500μMMethylglyoxalisincubatedwith100μMBSAdissolvedinphosphatebufferedsaline(PBS)for24hours,thenwashedon10kDafilterstoremoveexcessmethylglyoxal,reconstitutedwithDMEM/F12serumfreemediaandpassedthrougha0.2μmicronfilter.TGF-β(5ng/mL)ispreparedtotreatcellsinasubsetofexperiments.Cellsareco-treatedwithoneorcombinationsofthefollowing:Angiotensin(1-7)(100nM),D-Ala7-Ang-(1-7)(10μM),ERK1/2kinaseinhibitor,PD98059(1μM),TGF-βreceptorkinaseinhibitor;SB525334(1μM),theAT₁receptorantagonistLosartan(1μM),therenininhibitorAliskerin(1μM)andtheACEinhibitorLisinopril(1μM)^[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Angiotensin1-7(Ang1-7)isdissolvedin0.9%saline(MiceandRat)^[3][4].

Mice^[3]
MaleandfemaleBALB/cmice(1:1ratio,6-10weeksold,meanweight20g.)areused.Angiotensinfragment1-7acetatesalthydrate(Ang1-7)isdissolvedin0.9%saline(vehicle)at1mg/mLandstoredat-80°C.Variousdoses(0.01,0.06,0.1,0.3and1mg/kg)arefreshlypreparedfromthestockeachdayoftheexperiment,andadministeredtomicebydailyintra-peritoneal(i.p)injectionsinavolumeof500μLperinjection,eitherbefore(prophylacticapproach)orafter(treatmentapproach)DSStreatment.A779(MAS-1Rantagonist)issimilarlydissolvedindistilledwaterat1mg/mLandstoredat-80°C.Afreshlyprepareddoseof1mg/kgisadministeredtoasecondgroupofmicebydailyi.pinjectionsinavolumeof500μLdaily(for4days)alongwithcolitisinduction(prophylacticapproach).AthirdgroupofmicereceiveDSScontainingwateranddailyi.pinjectionsof0.9%saline(vehicle).ThefourthgroupreceiveDSScontainingwateralongwithdailyi.pinjectionswithDexamethasone(DEX)atdosesof0.01-1.0mg/kgoritsvehicle(0.9%saline)(prophylacticapproach).
Rat^[4]
TwentysixovariectomizedfemaleWistarratsweighing200±20gareused.Angiotensin(1-7)isadministeredintravenouslybyamicrosyringepumpattwodifferentcontinuousdosesof100and300ng/kg/minafterantagonist/salineinfusion.Eachdoseisinfusedfor15min;andMAP,RPP,andRBFarerecordedduringAngiotensin(1-7)infusionandthelast3-5minofeachdosemeasuredas“responsetoAngiotensin(1-7)infusion”.DuringAngiotensin(1-7)infusion,RPPissustainedatpre-Ang1-7infusionlevelsviaanadjustableaorticclamp.Attheendoftheexperiment,theratsarehumanelykilledbyanestheticoverdose,andtheleftkidneysareremovedandweighedimmediately.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].LiP,etal.Angiotensin-(1-7)augmentsbradykinin-inducedvasodilationbycompetingwithACEandreleasingnitricoxide.Hypertension.1997Jan;29(1Pt2):394-400.

  [2].AlzayadnehEM,etal.Angiotensin-(1-7)abolishesAGE-inducedcellularhypertrophyandmyofibroblasttransformationviainhibitionofERK1/2.CellSignal.2014Sep19.pii:S0898-6568(14)00314-3.

  [3].KhajahMA,etal.Anti-InflammatoryActionofAngiotensin1-7inExperimentalColitis.PLoSOne.2016Mar10;11(3):e0150861.

  [4].SaberiS,etal.RoleofMasreceptorinrenalbloodflowresponsetoangiotensin-(1-7)inovariectomizedestradioltreatedrats.ResPharmSci.2016Jan-Feb;11(1):65-72.

899.0

C₄₁H₆₂N₁₂O₁₁

51833-78-4

RoomtemperatureincontinentalUS;mayvaryelsewhere

H₂O:≥30.2mg/mL

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

Purity:98.62%

SelectBatch:HY-12403-13511

DataSheet(131KB)SDS(120KB)

COA(99KB)LCMS(104KB)

HandlingInstructions(1252KB)

• [1].LiP,etal.Angiotensin-(1-7)augmentsbradykinin-inducedvasodilationbycompetingwithACEandreleasingnitricoxide.Hypertension.1997Jan;29(1Pt2):394-400.

  [2].AlzayadnehEM,etal.Angiotensin-(1-7)abolishesAGE-inducedcellularhypertrophyandmyofibroblasttransformationviainhibitionofERK1/2.CellSignal.2014Sep19.pii:S0898-6568(14)00314-3.

  [3].KhajahMA,etal.Anti-InflammatoryActionofAngiotensin1-7inExperimentalColitis.PLoSOne.2016Mar10;11(3):e0150861.

  [4].SaberiS,etal.RoleofMasreceptorinrenalbloodflowresponsetoangiotensin-(1-7)inovariectomizedestradioltreatedrats.ResPharmSci.2016Jan-Feb;11(1):65-72.

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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