VU0467154-DataSheet-生命科學(xué)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(diǎn):mAChR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:13.89mg/mL(31.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2500mL11.2499mL22.4997mL5mM0.4500mL2.2500mL4.4999mL10mM0.2250mL1.1250mL2.2500mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)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(diào)節(jié)劑，能夠增強(qiáng)??，?和?蟹猴M4受體對(duì)?酰膽堿的反應(yīng)，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(nèi)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(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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