Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemERopivacainemesylateCat.No.:HY-B0563CCASNo.:854056-07-8分?式:C??H??N?O?S分?量:370.51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)H2O:250mg/mL(674.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.6990mL13.4949mL26.9898mL5mM0.5398mL2.6990mL5.3980mL10mM0.2699mL1.3495mL2.6990mL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Ropivacainemesylate?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(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在動(dòng)物實(shí)驗(yàn)?zāi)Ｐ椭?，?于局部?醉和神經(jīng)性疼痛的緩解。IC50&TargetIC50:sodiumioninflux[1]IC50:402.7μM(TREK-1inCOS-7cell'smembrane)[3]1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE體內(nèi)研究EpiduraladministrationofRopivacainemesylateeffectivelyblocksneuropathicpain(bothmechanicalallodyniaandheathyperalgesia)withoutinductionofanalgesictoleranceandsignificantlydelaysthedevelopmentofneuropathicpainproducedbyperipheralnerveinjury[1].Ropivacainemesylateinhibitspressure-inducedincreasesinfiltrationcoefficient(Kf)withoutaffectingpulmonaryarterypressure(Ppa),pulmonarycapillarypressures(Ppc),andzonalcharacteristics(ZC)[2].Ropivacainemesylatepreventspressure-inducedlungedemaandassociatedhyperpermeabilityasevidencebymaintainingPaO2,lungwet-to-dryratioandplasmavolumeinlevelssimilartoshamrats[2].Ropivacainemesylateinhibitspressure-inducedNOproductionasevidencedbydecreasedlungnitro-tyrosinecontentwhencomparedtohypertensivelungs[2].AnimalModel:AdultSprague-Dawleyrats(300-400g)[2]Dosage:1μMAdministration:Infusion(addedtotheperfusatereservoir)Result:Attenuatedpressure-dependentincreasesinfiltrationcoefficient(Kf).REFERENCES[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.JAnesth.2014Feb;28(1):81-6.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapp