Alprenolol-RS-Alprenolol-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAlprenololCat.No.:HY-B1517CASNo.:13655-52-2Synonyms:(RS)-Alprenolol;dl-Alprenolol分⼦式:C₁₅H₂₃NO₂分⼦量:249.35作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2years*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验DMSO:100mg/mL(401.04mM;Needultrasonic)H2O:0.67mg/mL(2.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.0104mL20.0521mL40.1043mL5mM0.8021mL4.0104mL8.0209mL10mM0.4010mL2.0052mL4.0104mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤.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：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(10.03mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(10.03mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(10.03mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:4mg/mL(16.04mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY⽣物活性Alprenolol((RS)-Alprenolol;dl-Alprenolol)⼀种具有⼝服活性的⾮选择性β-肾上腺素受体(β-adrenoceptor)拮抗剂，也5-HT1A和5-HT1B受体的拮抗剂。Alprenolol可⽤作抗⾼⾎压、抗⼼绞痛和抗⼼律失常剂。IC50&Target5-HT1AReceptor体内研究Alprenolol(p.o.,50mg/kg)causesasignificantdropinbloodpressurewhichaverages20mmHg(at3-hr)andanincreaseinheartrateby39beats/min(at3-hr)inconsciousrenalhypertensivedogs[1].Alprenolol(i.p.,5mg/kg)effectivelyblockestheanxiolyticeffectsofindorenateandipsapironebutdonotreducethemotoractivityinadultmaleSwissWebstermice[2].Alprenolol(intravenousinjection,0.5or1.0mg/kg)candecreasesystolicpressurebyameanof10mmHg,diastolicpressurebyameanof10mmHg)andheartrateby23beats/min,aswellasslightlyreducebothmyocardialandliverbloodflowsbymeanof17%and15%respectivelyatadoseof1.0mg/kgincats[3].户使⽤本产品发表的科研⽂献•NatCommun.2020Sep25;11(1):4857.•JPharmaceutBiomed.2020,113870.•bioRxiv.2020Jan.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HimoriN,etal.Effectsofbeta-adrenoceptorblockingagents,pindolol,alprenololandpractololonbloodpressureandheartrateinconsciousrenalhypertensivedogs.ArchIntPharmacodynTher.1977Jan;225(1):152-65.[2].Fernández-GuastiA,etal.Evidencefortheinvolvementofthe5-HT1Areceptorintheanxiolyticactionofindorenateandipsapirone.Psychopharmacology(Berl).1990;101(3):354-8.[3].ParrattJR,etal.Myocardialandhaemodynamiceffectsofthebeta-adrenoceptorblockingdrugalprenolol(H56/28)inanaesthetizedcats.BrJPharmacol.1969Oct;37(2):357-66.McePdfHeightCaution:Producthasnotbeenfullyvalidatedforme