Piromelatine-Neu-P11-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEPiromelatineCat.No.:HY-105285CASNo.:946846-83-9Synonyms:Neu-P11分⼦式:C₁₇H₁₆N₂O₄分⼦量:312.32作⽤靶点:MelatoninReceptor;5-HTReceptor;P2XReceptor;TRPChannel;SodiumChannel作⽤通路:GPCR/GProtein;NeuronalSignaling;MembraneTransporter/IonChannel储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:250mg/mL(800.46mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2018mL16.0092mL32.0184mL5mM0.6404mL3.2018mL6.4037mL10mM0.3202mL1.6009mL3.2018mL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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.66mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.66mM);Clearsolution1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Piromelatine(Neu-P11)褪⿊素受体MT1/MT2的激动剂，5-HT1A和5-HT1D的激动剂，也5-HT2B的拮抗剂。Piromelatine(Neu-P11)有⽤于促进睡眠、镇痛、抗神经退⾏性和抗抑郁等研究的潜能。Piromelatine(Neu-P11)还具有抑制疼痛相关靶点P2X3、TRPV1和Nav1.7通道的活性。IC50&TargetMT1MT25-HT1AReceptor5-HT1DReceptor(Agonist)(Agonist)5-HT2BReceptor(Antagonist)体内研究Piromelatine(20mg/kg,ip,daily)treatmentpreventsinsulinresistanceinducedbysleeprestriction[1].Piromelatine(5-50mg/kg,ip,daily)decreasesplasmaglucosesignificantly[2].Piromelatine(100mg/kg)decreasesthermalhyperalgesiaandmechanicalallodyniainPSL(partialsciaticnerveligation)mice[3].AnimalModel:TwentyfourmaleSprague-Dawleyrats(3monthsold,weighing250-300g)[1].Dosage:20mg/kg.Administration:IP,dailyat8:00p.m.Result:Resultedinsignificantlydecreasedplasmaglucoselevels(6.670.35mmol/L,6.770.34mmol/Lvs.8.270.38mmol/L),andtheplasmaglucoselevelsofthetwogroupswereevennearedtothatofthenormalcontrolgroup(6.07±0.35mmol/L).Resultedinadecreaseintriglyceridesandtotalcholesterollevels(51.8%and43.0%,respectively)andanelevationinHDL-Clevel(increaseof32.4%).AnimalModel:Fivegroupsof12-wk-oldrats(10/group)[2].Dosage:5-50mg/kg.Administration:Intraperitonealinjectionin18:00everyday.Result:Plasmaglucosewasdecreasedsignificantlyby27.3%,34.5%and61.5%,respectively.AnimalModel:MaleC57BL/6Jmice,weighing22-26g(10weeksold;PSLmice)[3].Dosage:25,50,or100mg/kg.Administration:IP1hbeforeassessmentofthermalhyperalgesiaandmechanicalallodynia.Result:Remarkablyprolongedthermallatency(surgery×treatmentinteraction,F1,24=15.7,p5,120=3.0,p1,24=18.4,p5,120=2.6,p<0.05)for4hafteradministrationofpiromelatinetoPSLmice.2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].MeihuaShe,etal.Piromelatine,aNovelMelatoninReceptorAgonist,StabilizesMetabolicProfilesandAmelioratesInsulinResistanceinChronicSleepRestrictedRats.EurJPharmacol.2014Mar15;727:60-5.[2].LHuang,etal.BloodPressureReducingEffectsofPiromelatineandMelatonininSpontaneouslyHypertensiveRats.EurRevMedPharmacolSci.2013Sep;17(18):2449-56.[3].Yuan-YuanLiu,etal.PiromelatineExertsAntinociceptiveEffectviaMelatonin,Opioid,and5HT1AReceptorsandHypnoticEffectviaMelatoninReceptorsinaMouseModelofNeuropathicPain.Psychopharmacology(Berl).2014Oct;231(20):3973-85.McePdfHeightCaution:Product