Quipazine-dimaleate-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEQuipazinedimaleateCat.No.:HY-101046CASNo.:150323-78-7分?式:C??H??N?O?分?量:445.42作?靶點(diǎn):5-HTReceptor;SARS-CoV作?通路:GPCR/GProtein;NeuronalSignaling;Anti-infection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:250mg/mL(561.27mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2451mL11.2254mL22.4507mL5mM0.4490mL2.2451mL4.4901mL10mM0.2245mL1.1225mL2.2451mL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%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.67mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Quipazinedimaleate5-HT的激動(dòng)劑，取代??內(nèi)?層中5-HT3R的[3H]GR65630的Ki值為1.4nM。Quipazinedimaleate對(duì)SARS-CoV-2具有抗病毒活性，EC50值為31.64μM。Quipazinedimaleate在外周模型中表現(xiàn)為5-HT3R的拮抗劑，可?于神經(jīng)疾病研究。體外研究Quipazinedimaleateshowsbindingefficacyto5-HT1and5-HT2withKivaluesof230nM[3].Quipazinedimaleatedisplaces[3H]GR65630from5-HT3RinratentorhinalcortexwithaKivalueof1.4nM[3].QuipazinedimaleateshowsantagonisticpropertiesontheratvagusnervewithpIC50valueof6.1,6.49and6.17for5-HT2,5-HT1andinhibitionof5-HTrelease[4].體內(nèi)研究Quipazinedimaleate(2.5,5and7.5mg/kg,onedoseforonce;i.p.)affectsdietaryself-selectionofdifferentmacronutrientdietsinmaleandfemalerats[1].AnimalModel:MaleandfemaleWistarratsfeedwithdifferentsourcesofthethreemacronutrients(Group1:casein,cornstarch,saffloweroil.Group2:eggprotein,cornstarch/sucrose,lard.GroupS:caseinhydrolysate,maltosedextrin,butter.)[1]Dosage:2.5,5and7.5mg/kgAdministration:Intraperitonealinjection;2.5,5and7.5mg/kg,onedoseforonceResult:IncreasedwaterintakeandfoodintakeofmaleratsfromGroupS,andreducedfoodintakeoffemaleratsfromGroup1andGroup2sat2hpost-injection.ReducedfoodintakeinfemaleratsfromGroup2,reducedproteinintakeinfemaleratsfromGroup1.REFERENCES[1].MokE,etal.Effectofquipazine,aselective5-HT3agonist,ondietaryself-selectionofdifferentmacronutrientdietsinmaleandfemalerats.Appetite.2000Jun;34(3):313-25.[2].GüntherS,etal.X-rayscreeningidentifiesactivesiteandallostericinhibitorsofSARS-CoV-2mainprotease.Science.2021May7;372(6542):642-646.[3].GlennonRA,etal.5-HT1and5-HT2bindingcharacteristicsofsomequipazineanalogues.JMedChem.1986Nov;29(11):2375-80.[4].IrelandSJ,TyersMB.Pharmacologicalcharacterizationof5-hydroxytryptamine-induceddepolarizationoftheratisolatedvagusnerve.BrJPharmacol.1987Jan;90(1):229-38.McePdfHeightCaution:Producthasnotbeenfullyvalidatedf