MK-1064-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMK-1064Cat.No.:HY-19914CASNo.:1207253-08-4分⼦式:C₂₄H₂₀ClN₅O₃分⼦量:461.9作⽤靶点:OrexinReceptor(OXReceptor)作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(108.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1650mL10.8249mL21.6497mL5mM0.4330mL2.1650mL4.3299mL10mM0.2165mL1.0825mL2.1650mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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(5.41mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性MK-1064⼀种选择性的、具有⼝服活性的OX2R拮抗剂(Ki:0.5nM,IC50:18nM)。MK-1064可促进睡眠(invivo)。MK-1064可⽤于神经相关的研究。IC50&TargetOX2ReceptorOX1ReceptorOX2ReceptorOX1Receptor18nM(IC50)1789nM(IC50)0.5nM(Ki)1584nM(Ki)体内研究MK-1064(30ꢀmg/kg,oraladministration)promotessleepinrodentsselectivelythroughOX2RinWild-typemice[2].MK-1064(30ꢀmg/kg,oraladministration,5days)reversesthestrugglebehaviorinducedbyCNOpre-treatmentinrats[3].MK-1064(1-5mg/kg,intravenousinjection/oraladministration)showsmoderateoralbioavailabilityandclearanceinrat,dog,andrhesusmonkey[1].AnimalModel:Wild-typeandOX2Rknockoutmice[2]Dosage:30mg/kgAdministration:OraladministrationResult:DisplayedactivewakereductionaccompaniedbysignificantincreasesinSWS(slow-wavesleep)andREM(rapideyemovement)attimepointsupto3.5ꢀhoursfollowingtreatment.AnimalModel:Rat,dog,andrhesusmonkey(Pharmacokineticsassay)[1]Dosage:1,2,3,5mg/kgAdministration:Oraladministration(P.O.),intravenousinjection(I.V.)Result:PharmacokineticsprofileofMK-1064.SpeciesDose(mg/kg)CL(mL/min/kg)t1/2(h)Dose(mg/kg)Cmax(μM)F(%)Rat2(I.V.)390.35(P.O.)1.554Dog1(I.V.)161.03(P.O.)1.048Rhesus2(I.V.)120.85(P.O.)0.916户使⽤本产品发表的科研⽂献•Neuropharmacology.17June2022,109168.•Neuropharmacology.2018Dec;143:79-94.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].RoeckerAJetal.Discoveryof5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide(MK-1064):aselectiveorexin2receptorantagonist(2-SORA)forthetreatmentofinsomnia.ChemMedChem.2014Feb;9(2):311-22.[2].GotterALetal.Orexin2ReceptorAntagonismisSufficienttoPromoteNREMandREMSleepfromMousetoMan.SciRep.2016Jun3;6:27147.[3].LauraAGrafe,etal.Orexin2receptorregulationofthehypothalamic-pituitary-adrenal(HPA)responsetoacuteandrepeatedstress.Neuroscience.2017Apr21;348:313-323.McePdfHeightCaution:Producthasnotbeenfullyvalidated