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

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.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)扫描⼆维码，DMSO:6.8mg/mL(27.79mM;Needultrasonicand运⽤溶解⽅案计算器warming)获得适合您实验体系的溶解⽅案*"≥"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%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.08mg/mL(8.50mM);Clearsolution1/4www.MedChemEwww.MedChemE此⽅案可获得≥2.08mg/mL(8.50mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述2.体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。请依序添加每种溶剂：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(8.50mM);Clearsolution此⽅案可获得≥2.08mg/mL(8.50mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶3.液中，混合均匀。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥2.08mg/mL(8.50mM);Clearsolution此⽅案可获得≥2.08mg/mL(8.50mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。4.以1mL⼯作液为例，取100μL20.8mg/mL的澄请依序添加每种溶剂：PBSDMSO储备液加到900μL⽟⽶油中，混合均匀。Solubility:130mg/mL(531.22mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性PilocarpineHydrochloride⼀种选择性的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<0.01or0.05),whilethatofHCScellstreatedwithPilocarpinebelowtheconcentrationof0.625g/Lshownosignificantdifferencetocontrols[2].Thepartialmuscarinicagonist,Pilocarpine,evokesconcentration-dependentrelaxationwithanEC50of2.4mMinisolatedsegmentsofrattailarterythatwereconstrictedwithPenylephrine(10to200nM)[3].体内研究ThePilocarpine-inducedsalivasecretionofthecontrolrats(CN)andexercised(EX)ratsisexamined.AsignificantlygreateramountofsalivaisinducedbyPilocarpineintheEXratsthanintheCNrats(P<0.01).Conversely,theNa+concentrationinthesalivaoftheEXratsissignificantlylowerthanthatoftheCNrats(P<0.05)[1].PROTOCOLCellAssay[2]CellviabilityisdeterminedbyMTTassay.Briefly,HCScellsareinoculatedintoa96-wellcultureplate(Nunc)atadensityof1×104cells/100µL/well,andareculturedandtreated.Ata4hinterval,thePilocarpine2/4www.MedChemEwww.MedChemE(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,preweighedcottonwasplacedintheirmouthssublingually,andPilocarpine(0.5mg/kg)isintraperitoneallyinjectedtoinducesalivasecretion.Eachcottonballisthenchangedevery10minfor1h.Thecollectedcottonballsareweighedagain,andthemassofsalivasecretediscalculatedbysubtractingtheinitialfromthefinalweight.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Neuropharmacology.2017May1;117:238-248.•CellMolNeurobiol.2020Oct15.•Neuroscience.2020Nov13.•JMolNeurosci.2020Nov;70(11):1858-1870.•EpilepsyRes.2018May;142:45-52.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-inducedrelaxationofrattailarterybya