Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMaropitantCat.No.:HY-10053CASNo.:147116-67-4分?式:C??H??N?O分?量:468.67作?靶點(diǎn):NeurokininReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:33.33mg/mL(71.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1337mL10.6685mL21.3370mL5mM0.4267mL2.1337mL4.2674mL10mM0.2134mL1.0668mL2.1337mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.33mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Maropitant?種選擇性的具有?服活性的神經(jīng)激肽(NK1)受體拮抗劑。Maropitant通過阻?催吐中?與化學(xué)感受器觸發(fā)區(qū)(CRTZ)中P物質(zhì)的結(jié)合?起作?。Maropitant在預(yù)防嘔吐??常有效。體內(nèi)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