Quipazine-dimaleate-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEQuipazinedimaleateCat.No.:HY-101046CASNo.:150323-78-7分⼦式:C₂₁H₂₃N₃O₈分⼦量:445.42作⽤靶点:5-HTReceptor;SARS-CoV作⽤通路:GPCR/GProtein;NeuronalSignaling;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(561.27mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2451mL11.2254mL22.4507mL5mM0.4490mL2.2451mL4.4901mL10mM0.2245mL1.1225mL2.2451mL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%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.67mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Quipazinedimaleate5-HT的激动剂，取代⼤⿏内⽪层中5-HT3R的[3H]GR65630的Ki值为1.4nM。Quipazinedimaleate对SARS-CoV-2具有抗病毒活性，EC50值为31.64μM。Quipazinedimaleate在外周模型中表现为5-HT3R的拮抗剂，可⽤于神经疾病研究。体外研究Quipazinedimaleateshowsbindingefficacyto5-HT1and5-HT2withKivaluesof230nM[3].Quipazinedimaleatedisplaces[3H]GR65630from5-HT3RinratentorhinalcortexwithaKivalueof1.4nM[3].QuipazinedimaleateshowsantagonisticpropertiesontheratvagusnervewithpIC50valueof6.1,6.49and6.17for5-HT2,5-HT1andinhibitionof5-HTrelease[4].体内研究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