Maropitant-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMaropitantCat.No.:HY-10053CASNo.:147116-67-4分⼦式:C₃₂H₄₀N₂O分⼦量:468.67作⽤靶点:NeurokininReceptor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:33.33mg/mL(71.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1337mL10.6685mL21.3370mL5mM0.4267mL2.1337mL4.2674mL10mM0.2134mL1.0668mL2.1337mL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>>90%cornoilSolubility:≥2.5mg/mL(5.33mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Maropitant⼀种选择性的具有⼝服活性的神经激肽(NK1)受体拮抗剂。Maropitant通过阻⽌催吐中⼼与化学感受器触发区(CRTZ)中P物质的结合⽽起作⽤。Maropitant在预防呕吐⽅⾮常有效。体内研究Treatmentwith1mg/kgMaropitantcitrate,significantlyreducesthesizeofulcerativedermatitis(UD)lesionsinmice.IntravenousMaropitantdecreasesMACby16%.Incontrast,epiduraladministrationofeithersalineorMaropitantdoesnotchangetheMAC(2.17%and1.92%,respectively).REFERENCES[1].HayKrausBL.Efficacyofmaropitantinpreventingvomitingindogspremedicatedwithhydromorphone.VetAnaesthAnalg.2013Jan;40(1):28-34.[2].LesmanSP,BoucherJF,GroverGS,etal.Thepharmacokineticsofmaropitantcitratedosedorallytodogsat2mg/kgand8mg/kgoncedailyfor14daysconsecutivedays.JVetPharmacolTher.2012Nov20.[3].AlvillarBM,BoscanP,MamaKR,etal.Effectofepiduralandintravenoususeoftheneurokinin-1(NK-1)receptorantagonistmaropitantonthesevofluraneminimumalveolarconcentration(MAC)indogs.VetAnaesthAnalg.2012Mar;39(2):201-5.[4].RamseyDS,KincaidK,WatkinsJAetal.Safetyandefficacyofinjectableandoralmaropitant,aselectiveneurokinin1receptorantagonist,inarandomizedclinicaltrialfortreatmentofvomitingindogs.JVetPharmacolTher.2008Dec;31(6):538-43.doi[5].BenchaouiHA,CoxSR,SchneiderRPetal.Thepharmacokineticsofmaropitant,anovelneurokinintype-1receptorantagonist,indogs.JVetPharmacolTher.2007Aug;30(4):336-44.[6].MaropitantMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For