Icatibant-HOE-140-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIcatibantCat.No.:HY-17446CASNo.:130308-48-4Synonyms:HOE140分⼦式:C₅₉H₈₉N₁₉O₁₃S分⼦量:1304.52作⽤靶点:BradykininReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:100mg/mL(76.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.7666mL3.8328mL7.6657mL5mM0.1533mL0.7666mL1.5331mL10mM0.0767mL0.3833mL0.7666mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：PBSSolubility:50mg/mL(38.33mM);Clearsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Icatibant(HOE-140)有效的，特异的缓激肽B2受体拮抗剂，IC50和Ki值分别为1.07nM和0.798nM。体外研究Icatibant(10-30μM)potentiatesangiotensinIII,butnotangiotensinII(contractionmediatedbyangiotensinAT1receptors),andLys-des-Arg9-bradykinin,butnotdes-Arg9-bradykinin(effectsmediatedbythebradykininB1receptors)[3].体内研究Icatibant(0.3,or1.5mg/kg,subcutaneousadministrationtwicedailyinmice)showsasignificantpreventiveeffectonulcerativeColitis[2].AnimalModel:FemalemiceoftheCBA/J(H-2k)strain[2].Dosage:0.06,0.3,or1.5mg/kg.Administration:Subcutaneousadministrationtwicedaily.Result:Thelengthofthelargeintestinewas93.6±6.8mmwiththe1.5mg/kgdosageand94.0±4.1mmwiththe0.3mg/kgdosage,showingasignificantpreventiveeffectonshortening.户使⽤本产品发表的科研⽂献•AdvSci(Weinh).2022Oct18;e2203088.•SciRep.2020Aug25;10(1):14160.•BiochemBiophysResCommun.2016Apr29;473(2):396-402.•JReninAngiotensinAldosteroneSyst.14Jun2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HockFJ,etal.Hoe140anewpotentandlongactingbradykinin-antagonist:invitrostudies.BrJPharmacol.1991Mar;102(3):769-73.[2].YArai,etal.EffectofIcatibant,aBradykininB2ReceptorAntagonist,ontheDevelopmentofExperimentalUlcerativeColitisinMice.DigDisSci.1999Apr;44(4):845-51.[3].Marie-ThérèseBawolak,etalTheBradykininB2ReceptorAntagonistIcatibant(Hoe140)BlocksAminopeptidaseNatMicromolarConcentrations:Off-TargetAlterationsofSignalingMediatedbytheBradykininB1andAngiotensinReceptors.EurJPharmacol.2006McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication