Metipranolol-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrariesMetipranololCat.No.:HY-121567CASNo.:22664-55-7分⼦式:C₁₇H₂₇NO₄分⼦量:309.4作⽤靶点:AdrenergicReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfromlight)溶解性数据体外实验DMSO:250mg/mL(808.02mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2321mL16.1603mL32.3206mL5mM0.6464mL3.2321mL6.4641mL10mM0.3232mL1.6160mL3.2321mL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。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%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.08mg/mL(6.72mM);Clearsolution此⽅案可获得≥2.08mg/mL(6.72mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述2.体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。请依序添加每种溶剂：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.72mM);Clearsolution此⽅案可获得≥2.08mg/mL(6.72mM，饱和度未知)的澄溶液。1/3以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶3.液中，混合均匀。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥2.08mg/mL(6.72mM);Clearsolution此⽅案可获得≥2.08mg/mL(6.72mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。BIOLOGICALACTIVITY⽣物活性Metipranolol⼀种⾮选择性的具有⼝服活性的β-肾上腺素能受体(β-adrenergicreceptor)拮抗剂。Metipranolol可⽤于⾼⾎压和光眼的研究。IC50&Targetβ1adrenoceptorβ2adrenoceptor8.3(pA2)8.4(pA2)体外研究Invitroβ1-andβ2-adrenoceptorantagonismisevaluatedusingtheguineapigatriumandtheratuterus,respectively.TherespectivepA2valuesare8.3and8.4[2].Metipranololsignificantlyreducesiron/ascorbate-inducedlipidperoxidationinratbrainhomogenateswithanIC50valueof6.9μM.Metipranololalsoconcentration-dependentlyinhibitssodiumnitroprusside-stimulatedlipidperoxidationinratbrainhomogenates,displayinganIC50valueof25.1μM[3].体内研究Atpostnatalday35(P35),rd10micegivendailysubcutaneousinjectionsof40mg/kgofMetipranololhasreductioninmarkersofnitrosativestress,fewerTUNEL-positivecells,increasedouternuclearlayerthickness,andsubstantiallymorestainingforrhodopsin.AtP50,Metipranolol-treatedrd10micehasdecreased3-nitrotyrosinestainingintheretina,increasedimmunostainingforconearrestin,amarkerforconephotoreceptors,andsignificantlyhigherscotopicandphotopicb-waveamplitudesatthehigheststimulusintensity.AtP65,conedensityissignificantlyhigherinMetipranolol-treatedversusvehicle-injectedrd10mice[1].REFERENCES[1].YogitaKanan,etal.Metipranololpromotesstructureandfunctionofretinalphotoreceptorsintherd10mousemodelofhumanretinitispigmentosa.JNeurochem.2019Jan;148(2):307-318.[2].MFSugrue,etal.Astudyontheocularandextraocularpharmacologyofmetipranolol.GraefesArchClinExpOphthalmol.1985;222(3):123-7.[3].JoséMelena,etal.Metipranololattenuateslipidperoxidationinratbrain:acomparativestudywithotherantiglaucomadrugs.GraefesArchClinExpOphthalmol.2003Oct;241(10):827-33.MceP