Ropivacaine-DataSheet-生命科學(xué)試劑-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemERopivacaineCat.No.:HY-B0563CASNo.:84057-95-4分?式:C??H??N?O分?量:274.4作?靶點(diǎn):SodiumChannel;PotassiumChannel作?通路:MembraneTransporter/IonChannel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:12.5mg/mL(45.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.6443mL18.2216mL36.4431mL5mM0.7289mL3.6443mL7.2886mL10mM0.3644mL1.8222mL3.6443mL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，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。BIOLOGICALACTIVITY?物活性Ropivacaine?種有效的鈉通道(sodiumchannel)阻斷劑，可以作為局部?醉試劑。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(dǎo)阻滯。Ropivacaine也?種K2P(雙孔鉀通道)TREK-1的抑制劑，在COS-7細(xì)胞膜上的IC50值為402.7μM。Ropivacaine?于局部?醉和神經(jīng)性疼痛的緩解的相關(guān)研究。IC50&TargetIC50:sodiumioninflux[1]IC50:402.7μM(TREK-1inCOS-7cell'smembrane)[2]1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE體內(nèi)研究EpiduraladministrationofRopivacaineeffectivelyblocksneuropathicpain(bothmechanicalallodyniaandheathyperalgesia)withoutinductionofanalgesictoleranceandsignificantlydelaysthedevelopmentofneuropathicpainproducedbyperipheralnerveinjury[1].Ropivacaineinhibitspressure-inducedincreasesinfiltrationcoefficient(Kf)withoutaffectingpulmonaryarterypressure(Ppa),pulmonarycapillarypressures(Ppc),andzonalcharacteristics(ZC)[2].Ropivacainepreventspressure-inducedlungedemaandassociatedhyperpermeabilityasevidencebymaintainingPaO2,lungwet-to-dryratioandplasmavolumeinlevelssimilartoshamrats[2].Ropivacaineinhibitspressure-inducedNOproductionasevidencedbydecreasedlungnitro-tyrosinecontentwhencomparedtohypertensivelungs[2].AnimalModel:AdultSprague-Dawleyrats(300–400g)[1]Dosage:1μMAdministration:Infusion(addedtotheperfusatereservoir)Result:Attenuatedpressure-dependentincreasesinfiltrationcoefficient(Kf).?ResearchSquarePreprint.2020Oct.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LiTF,etal.Epiduralsustainedreleaseropivacaineprolongsanti-allodyniaandanti-hyperalgesiaindevelopingandestablishedneuropathicpain.PLoSOne.2015Jan24;10(1):e0117321.[2].MilanPatel,etal.RopivacaineInhibitsPressure-InducedLungEndothelialHyperpermeabilityinModelsofAcuteHypertension.LifeSci.2019Apr1;222:22-28.[3].DeneSimpson,etal.Ropivacaine:areviewofitsuseinregionalanaesthesiaandacutepainmanagement.Drugs.2005;65(18):2675-717.[4].HyeWonShin,etal.Theinhibitoryeffectsofbupivacaine,levobupivacaine,andropivacaineonK2P(two-poredomainpotassium)channelTREK-1.JAnesthMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap