Pilocarpine-Hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPilocarpineHydrochlorideCat.No.:HY-B0726CASNo.:54-71-7分⼦式:C₁₁H₁₇ClN₂O₂分⼦量:244.72作⽤靶点:mAChR作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,sealedstorage,awayfrommoisture*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验H2O:≥37mg/mL(151.19mM)DMSO:31.25mg/mL(127.70mM;ultrasonicandwarmingandheatto80°C)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM4.0863mL20.4315mL40.8630mL5mM0.8173mL4.0863mL8.1726mL10mM0.4086mL2.0432mL4.0863mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤.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:≥2.08mg/mL(8.50mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(8.50mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(8.50mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:130mg/mL(531.22mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性PilocarpineHydrochloride⼀种有效的M3型毒蕈碱⼄酰胆碱受体(M3muscarinicreceptor)激动剂。IC50&TargetM3muscarinicreceptor[1]体外研究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].体内研究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—您⾝边的抑制剂⼤师www.MedChemEplacedintheirmouthssublingually,andPilocarpine(0.5mg/kg)isintraperitoneallyinjectedtoinducesalivasecretion.Eachcottonballisthenchangedevery10minfor1h.Thecollectedcottonballsareweighedagain,andthemassofsalivasecretediscalculatedbysubtractingtheinitialfromthefinalweight.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•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