Palosuran-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrariesPalosuranhydrochlorideCat.No.:HY-10655ACASNo.:2469274-58-4分⼦式:C₂₅H₃₁ClN₄O₂分⼦量:454.99作⽤靶点:UrotensinReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:50mg/mL(109.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1979mL10.9893mL21.9785mL5mM0.4396mL2.1979mL4.3957mL10mM0.2198mL1.0989mL2.1979mL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，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性Palosuranhydrochloride(ACT-058362hydrochloride)⼀种有效，选择性和具有⼝服活性的urotensinIIreceptor受体拮抗剂，对于表达⼈重组受体的CHO细胞膜的IC50值为3.6nM。Palosuranhydrochloride可改糖尿病⼤⿏的胰腺和肾脏功能。IC50&TargetIC50:3.6nM(humanurotensinIIreceptor)[1]体外研究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].体内研究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).户使⽤本产品发表的科研⽂献•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)只为