VU0467154-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVU0467154Cat.No.:HY-112209CASNo.:1451993-15-9分⼦式:C₁₇H₁₅F₃N₄O₃S₂分⼦量:444.45作⽤靶点:mAChR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:13.89mg/mL(31.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2500mL11.2499mL22.4997mL5mM0.4500mL2.2500mL4.4999mL10mM0.2250mL1.1250mL2.2500mL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:1.39mg/mL(3.13mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性VU0467154⼀种M4毒蕈碱的⼄酰胆碱受体(M4muscarinicacetylcholinereceptor(mAChR))的正向调节剂，能够增强⼩⿏，⼈和⾷蟹猴M4受体对⼄酰胆碱的反应，pEC50值分别为7.75，6.2和6。IC50&TargetpEC50:of7.75(RatM4receptor),6.2(HumanM4receptor),6(CynomolgusmonkeyM4receptor)[1]体外研究VU0467154isapositiveallostericmodulatorsoftheM4muscarinicacetylcholinereceptor(mAChR),robustlypotentiatestheresponsetoAChwithpEC50sof7.75,6.2and6forrat,humanandcynomolgusmonkey(cyno)M4receptor,respectively.VU0467154doesnotpotentiatetheAChresponseatratandhumanM1,M2,M3,orM5[1].体内研究VU0467154(1-56.6mg/kg,p.o.ori.p.)reversesamphetamine-inducedhyperlocomotioninrats.VU0467154(0.3-30mg/kg,i.p.)reversesamphetamine-andMK-801-inducedhyperlocomotioninwild-typebutnotM4KOmice.VU0467154alonealsoenhancestheacquisitionofbothcontextualandcue-mediatedfearconditioninginwild-typemice[1].PROTOCOLAnimalRats[1]Administration[1]TodeterminetherelationshipbetweeninvivoefficacyofVU0467154andbrainconcentrationsinrats,theefficacyofVU0467154(1,3,10,30,and56.6mg/kg,PO;n≥8perdoselevel)inreversingamphetamine-inducedhyperlocomotioniscorrelatedtothebrainconcentrationsofVU0467154inthesameanimalsuponstudycompletion(1.5hpostadministration).Inmice,theinvivoconcentration-effectrelationshipforVU0467154isdeterminedbycorrelatingtheefficacyofVU0467154inreversingamphetamine-inducedhyperlocomotion(0.3,1,3,10,and30mg/kg,IP)tothebrainconcentrationsofVU0467154inthesameanimalsuponstudycompletion(2.5hpostadministration).Terminalunboundbrainconcentrationsforalltreatmentgroupsareplottedversuseachanimal’sefficacyinreversingamphetamine-inducedhyperlocomotion.NonlinearregressionanalysisoftheplotteddataarecalculatedtodeterminetheinvivoEC50value(nM)forVU0467154inreversingamphetamine-inducedhyperlocomotioninratsusingGraphPadPrism5.0[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•iScience.4October2022,105263.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BubserM,etal.SelectiveactivationofM4muscarinicacetylcholinereceptorsreversesMK-801-inducedbehavioralimpairmentsand2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEenhancesassociativelearninginrodents.ACSChemNeurosci.2014Oct15;5(10):920-42.McePdfHeightCaution:Producthasno