Icatibant-HOE-140-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIcatibantCat.No.:HY-17446CASNo.:130308-48-4Synonyms:HOE140分?式:C??H??N??O??S分?量:1304.52作?靶點(diǎn):BradykininReceptor作?通路:GPCR/GProtein儲(chǔ)存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:100mg/mL(76.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM0.7666mL3.8328mL7.6657mL5mM0.1533mL0.7666mL1.5331mL10mM0.0767mL0.3833mL0.7666mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：PBSSolubility:50mg/mL(38.33mM);Clearsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Icatibant(HOE-140)有效的，特異的緩激肽B2受體拮抗劑，IC50和Ki值分別為1.07nM和0.798nM。體外研究Icatibant(10-30μM)potentiatesangiotensinIII,butnotangiotensinII(contractionmediatedbyangiotensinAT1receptors),andLys-des-Arg9-bradykinin,butnotdes-Arg9-bradykinin(effectsmediatedbythebradykininB1receptors)[3].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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