VU0467154-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVU0467154Cat.No.:HY-112209CASNo.:1451993-15-9分?式:C??H??F?N?O?S?分?量:444.45作?靶點:mAChR作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:13.89mg/mL(31.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2500mL11.2499mL22.4997mL5mM0.4500mL2.2500mL4.4999mL10mM0.2250mL1.1250mL2.2500mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:1.39mg/mL(3.13mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性VU0467154?種M4毒蕈堿的?酰膽堿受體(M4muscarinicacetylcholinereceptor(mAChR))的正向調節(jié)劑，能夠增強??，?和?蟹猴M4受體對?酰膽堿的反應，pEC50值分別為7.75，6.2和6。IC50&TargetpEC50:of7.75(RatM4receptor),6.2(HumanM4receptor),6(CynomolgusmonkeyM4receptor)[1]體外研究VU0467154isapositiveallostericmodulatorsoftheM4muscarinicacetylcholinereceptor(mAChR),robustlypotentiatestheresponsetoAChwithpEC50sof7.75,6.2and6forrat,humanandcynomolgusmonkey(cyno)M4receptor,respectively.VU0467154doesnotpotentiatetheAChresponseatratandhumanM1,M2,M3,orM5[1].體內研究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.戶使?本產品發(fā)表的科研?獻?iScience.4October2022,105263.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BubserM,etal.SelectiveactivationofM4muscarinicacetylcholinereceptorsreversesMK-801-inducedbehavioralimpairmentsand2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEenhancesassociativelearninginrodents.ACSChemNeurosci.2014Oct15;5(10):920-42.McePdfHeightCaution:Producthasno