Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesPalosuranhydrochlorideCat.No.:HY-10655ACASNo.:2469274-58-4分?式:C??H??ClN?O?分?量:454.99作?靶點:UrotensinReceptor作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗H2O:50mg/mL(109.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1979mL10.9893mL21.9785mL5mM0.4396mL2.1979mL4.3957mL10mM0.2198mL1.0989mL2.1979mL請根據(jù)產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。BIOLOGICALACTIVITY?物活性Palosuranhydrochloride(ACT-058362hydrochloride)?種有效，選擇性和具有?服活性的urotensinIIreceptor受體拮抗劑，對于表達?重組受體的CHO細胞膜的IC50值為3.6nM。Palosuranhydrochloride可改糖尿病??的胰腺和腎臟功能。IC50&TargetIC50:3.6nM(humanurotensinIIreceptor)[1]體外研究Palosuran(8h)inhibits125I-U-IIbindingtohumanUTreceptor,withIC50sof46.2nMonTE671cellsand86nMonrecombinantCHOcells[1].PalosuraninhibitsCa2+mobilizationinresponsetohumanU-IIinCHOcellsexpressinghumanandratUTreceptorwithIC50sof17and>10000nM,respectively[1].1/3Palosuran(0.12-10000nM;20min)inhibitshumanU-IIinducedMAPKphosphorylationinadose-dependentmannerinrecombinantCHOcells,withanIC50of150nM[1].體內研究ACT-058362(10mg/kg/h;i.v.)fullypreventsthedecreaseinrenalbloodflowafterischemiainratswithoutdecreasingbloodpressure[1].Palosuran(300mg/kg/d;p.o.for16weeks)improvesthesurvival,increasesinsulin,andslowstheincreaseinglycemia,glycosylatedhemoglobin,andserumlipidsinstreptozotocin-induceddiabeticrats[2].AnimalModel:MaleWistarratswithrenalischemiaandreperfusion[1]Dosage:20mg/kg/hfor135minAdministration:I.v.(continuousinfusion)for135minResult:Restoredrenalbloodflowtobaselinevaluesat30minafterreperfusionandby60minincreasedrenalbloodflowby12%abovebaselinevalues.Didnotsignificantlyaltermeanarterialbloodpressure(MAP)andheartrate(HR).戶使?本產品發(fā)表的科研?獻?Endocrinology.2018May1;159(5):2253-2263.REFERENCES[1].ClozelM,et,al.Pharmacologyoftheurotensin-IIreceptorantagonistpalosuran(ACT-058362;1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-ureasulfatesalt):firstdemonstrationofapathophysiologicalroleoftheurotensinSystem.JPharmacolExpTher.2004Oct;311(1):204-12.[2].ClozelM,et,al.Theurotensin-IIreceptorantagonistpalosuranimprovespancreaticandrenalfunctionindiabeticrats.JPharmacolExpTher.2006Mar;316(3):1115-21.McePdfHeight2/3MedChemExpress(MCE)只為