Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERopivacainehydrochlorideCat.No.:HY-B0563BCASNo.:98717-15-8分?式:C??H??ClN?O分?量:310.86作?靶點:SodiumChannel;PotassiumChannel作?通路:MembraneTransporter/IonChannel儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:10mg/mL(32.17mM;Needultrasonic)H2O:10mg/mL(32.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.2169mL16.0844mL32.1688mL5mM0.6434mL3.2169mL6.4338mL10mM0.3217mL1.6084mL3.2169mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?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(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)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(xiàn)沉淀、析出現(xiàn)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:≥1mg/mL(3.22mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥1mg/mL(3.22mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1mg/mL(3.22mM);ClearsolutionBIOLOGICALACTIVITY?物活性Ropivacainehydrochloride?種有效的鈉通道(sodiumchannel)阻斷劑。Ropivacaine通過可逆地抑制鈉離?內(nèi)流(sodiumioninflux)從?引起神經(jīng)纖維脈沖傳導阻滯。Ropivacaine也?種K2P(雙孔鉀通道)TREK-1的抑制劑，在COS-7細胞膜上的IC50值為402.7μM。Ropivacaine在動物實驗模型中，可?于神經(jīng)性疼痛的緩解。IC50&TargetIC50:sodiumioninflux[1]IC50:402.7μM(TREK-1inCOS-7cell'smembrane)[3]體內(nèi)研究EpiduraladministrationofRopivacainehydrochlorideeffectivelyblocksneuropathicpain(bothmechanicalallodyniaandheathyperalgesia)withoutinductionofanalgesictoleranceandsignificantlydelaysthedevelopmentofneuropathicpainproducedbyperipheralnerveinjury[1].Ropivacainehydrochlorideinhibitspressure-inducedincreasesinfiltrationcoefficient(Kf)withoutaffectingpulmonaryarterypressure(Ppa),pulmonarycapillarypressures(Ppc),andzonalcharacteristics(ZC)[2].Ropivacainehydrochloridepreventspressure-inducedlungedemaandassociatedhyperpermeabilityasevidencebymaintainingPaO2,lungwet-to-dryratioandplasmavolumeinlevelssimilartoshamrats[2].Ropivacainehydrochlorideinhibitspressure-inducedNOproductionasevidencedbydecreasedlungnitro-tyrosinecontentwhencomparedtohypertensivelungs[2].AnimalModel:AdultSprague-Dawleyrats(300–400g)[2]Dosage:1μMAdministration:Infusion(addedtotheperfusatereservoir)Result:Attenuatedpressure-dependentincreasesinfiltrationcoefficient(Kf).戶使?本產(chǎn)品發(fā)表的科研?獻?StemCellResTher.2021Feb4;12(1):107.?EurSpineJ.2022Sep24.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LiTF,etal.Epiduralsustainedreleaseropivacaineprolongsanti-allodyniaandanti-hyperalgesiaindevelopingandestablishedneuropathicpain.PLoSOne.2015Jan24;10(1):e0117321.[2].MilanPatel,etal.RopivacaineInhibitsPressure-InducedLungEndothelialHyperpermeabilityinModelsofAcuteHypertension.LifeSci.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2019Apr1;222:22-28.[3].DeneSimpson,etal.Ropivacaine:areviewofitsuseinregionalanaesthesiaandacutepainmanagement.Drugs.2005;65(18):2675-717.[4].HyeWonShin,etal.Theinhibitoryeffectsofbupivacaine,levobupivacaine,andropivacaineonK2P(two-poredomainpotassium)channelTREK-1.JAnesth.2014Feb;28(1):81-6.McePdfHeightCaution:Producth