Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPilocarpineHydrochlorideCat.No.:HY-B0726CASNo.:54-71-7分?式:C??H??ClN?O?分?量:244.72作?靶點(diǎn):mAChR作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:≥37mg/mL(151.19mM)DMSO:31.25mg/mL(127.70mM;ultrasonicandwarmingandheatto80°C)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM4.0863mL20.4315mL40.8630mL5mM0.8173mL4.0863mL8.1726mL10mM0.4086mL2.0432mL4.0863mL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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?.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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(8.50mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(8.50mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(8.50mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:130mg/mL(531.22mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性PilocarpineHydrochloride?種有效的M3型毒蕈堿?酰膽堿受體(M3muscarinicreceptor)激動(dòng)劑。IC50&TargetM3muscarinicreceptor[1]體外研究ToevaluatethecytotoxicityofPilocarpine,themorphologyandviabilityofhumancornealstromal(HCS)cellsareexaminedbylightmicroscopyandMTTassay,respectively.MorphologicalobservationsshowthatHCScellsexposedtoPilocarpineataconcentrationfrom0.625to20g/Lexhibitdose-andtime-dependentproliferationretardationandmorphologicalabnormalitysuchascellularshrinkage,cytoplasmicvacuolation,detachmentfromculturematrix,andeventuallydeath,whilenoobviousdifferenceisobservedbetweenthoseexposedtoPilocarpinebelowtheconcentrationof0.625g/Landcontrols.ResultsofMTTassayrevealthatthecellviabilityofHCScellsdecreasewithtimeandconcentrationafterexposingtoPilocarpineabovetheconcentrationof0.625g/L(P[2].Thepartialmuscarinicagonist,Pilocarpine,evokesconcentration-dependentrelaxationwithanEC50of2.4mMinisolatedsegmentsofrattailarterythatwereconstrictedwithPenylephrine(10to200nM)[3].體內(nèi)研究ThePilocarpine-inducedsalivasecretionofthecontrolrats(CN)andexercised(EX)ratsisexamined.AsignificantlygreateramountofsalivaisinducedbyPilocarpineintheEXratsthanintheCNrats(P+concentrationinthesalivaoftheEXratsissignificantlylowerthanthatoftheCNrats(P[1].PROTOCOLCellAssay[2]CellviabilityisdeterminedbyMTTassay.Briefly,HCScellsareinoculatedintoa96-wellcultureplate(Nunc)atadensityof1×104cells/100μL/well,andareculturedandtreated.Ata4hinterval,thePilocarpine(0.625to20g/L)-containingmediumisreplacedentirelywith100μLserum-freeDMEM/F12mediumcontaining1.0g/LMTT,andthecellsareincubatedat37°Cinthedarkfor4h.AftertheMTT-containingmediumisdiscardedwithcaution,150μLDMSOisaddedtodissolvetheproducedformazancrystalsat37°Cinthedarkfor15min,andtheabsorbanceat490nmismeasuredwithaMultiskanGOmicroplatereader[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats[1]Administration[1]Male,10-week-oldWistarratsareassignedtooneoftwogroups,exercise(EX,n=6)andcontrol(CN,n=6).TheEXratsarekeptfor40daysincageswitharunningwheel(SN-451),allowingthemtoundertakevoluntaryexercise,whiletheCNratsarekeptincageswiththerunningwheellocked.Onthe40thday,Pilocarpine-inducedsalivaismeasuredasfollows.Briefly,theratsareanesthetized,preweighedcottonwas2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEplacedintheirmouthssublingually,andPilocarpine(0.5mg/kg)isintraperitoneallyinjectedtoinducesalivasecretion.Eachcottonballisthenchangedevery10minfor1h.Thecollectedcottonballsareweighedagain,andthemassofsalivasecretediscalculatedbysubtractingtheinitialfromthefinalweight.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Immunity.2022Jul12;S1074-7613(22)00291-6.?ProgNeurobiol.2022Aug2;102335.?FoodChem.30November2022,133593.?LifeSci.2022Nov1;308:120942.?IntImmunopharmacol.2022Aug22;111:109152.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MatsuzakiK,etal.Dailyvoluntaryexerciseenhancespilocarpine-inducedsalivasecretionandaquaporin1expressioninratsubmandibularglands.FEBSOpenBio.2017Dec7;8(1):85-93.[2].YuanXL,etal.Cytotoxicityofpilocarpinetohumancornealstromalcellsanditsunderlyingcytotoxicmechanisms.IntJOphthalmol.2016Apr18;9(4):505-11.[3].TontaMA,etal.Pilocarpine-inducedrelaxationofrattailarterybyanon-cholinergicmechanismandintheabsenceofanintactendothelium.BrJPharmacol.1994Jun;112(2):525-32.[4].WangRF,etal.Post-treatmentwiththeGLP-1analogueliraglutidealleviatechronicinflammationandmitochondrialstressinduce