Jatrorrhizine-hydroxide-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEJatrorrhizinehydroxideCat.No.:HY-N0749ACASNo.:483-43-2分?式:C??H??NO?分?量:355.38作?靶點(diǎn):AChE;5-HTReceptor;Bacterial作?通路:NeuronalSignaling;GPCR/GProtein;Anti-infection儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCOA.溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:5mg/mL(14.07mM;Needultrasonic)DMSO:3.33mg/mL(9.37mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.8139mL14.0694mL28.1389mL5mM0.5628mL2.8139mL5.6278mL10mM0.2814mL1.4069mL2.8139mL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Jatrorrhizinehydroxide從連中分離得到的?物堿，具有神經(jīng)保護(hù)、抗、抗瘧原?和抗氧化活性。Jatrorrhizinehydroxide有效的，具有?服活性的?酰膽堿酯酶(AChE)(IC50=872nM)的抑制劑，對(duì)BuChE的選擇性為115倍。Jatrorrhizinehydroxide通過(guò)抑制uptake-2transporter的活性減少?素(5-HT)和去甲腎上腺素(NE)的攝取。IC50&TargetIC50:872nM(AChE)[1]體外研究Jatrorrhizinehasantiplasmodialandantiamoebicactivity,itagainstPlasmodiumfalciparumandE.histolytica1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEwithIC50valuesof3.15and82.7μM,respectively[1].ThehOCT2(organiccationtransporter2),hOCT3,andPMAT(plasmamembranemonoaminetransporter)arecapableoftransportingmonoamineneurotransmittersinthebrain[3].Jatrorrhizinehastheinhibitorypotencyofjatrorrhizineon5-HTandNEuptakeinhOCT2-,hOCT3-,andPMAT-transfectedcells.JatrorrhizinestronglyinhibitsPMAT-mediatedMPP+uptakewithanIC50valueof1.05μMandreduces5-HTandNEuptakemediatedbyhOCT2,hOCT3,andhPMATwithIC50valuesof0.1-1μM(forOCT2andOCT3)and1-10μM(forPMAT)[3].Clearanceofneurotransmittersreleasedintothesynapticcleftisdefinedbytwodistinctprocesses.Uptake-1,thecommontargetofcurrentappliedantidepressants,iscomprisedoftheserotonintransporter(SERT),the“SERT”,hadahighaffinitybutlowcapacitytotakeup[3H]5-HT.Uptake-2transportersareanimportantsupplementaryregulationsysteminmonoamineclearancethoughttobethe“NET”,haslowaffinitybuthighcapacitytotakeup[3H]5-HTintobrainslices.Jatrorrhizinesignificantlyinhibited5-HTandNEuptakeinsynaptosomesat25μMand50μM[3].體內(nèi)研究Jatrorrhizine(intraperitonealinjection;5,10,20mg/kg)cansignificantlyreducethedurationofimmobilitywhencomparedwithvehiclecontrolgroupintailsuspensiontest(TST)[2].AnimalModel:MaleICRalbinomice[2]Dosage:5,10,20mg/kgAdministration:Intraperitonealinjection;5,10,20mg/kgResult:Reducedimmobilityperiodintailsuspensiontest.REFERENCES[1].SunS,etal.Jatrorrhizinereduces5-HTandNEuptakeviainhibitionofuptake-2transportersandproducesantidepressant-likeactioninmice.Xenobiotica.2019Oct;49(10):1237-1243.[2].XiaofeiJiang,etal.SynthesisandBiologicalEvaluationofNovelJatrorrhizineDerivativeswithAminoGroupsLinkedatthe3-PositionasInhibitorsofAcetylcholinesterase.ResearchArticleVolume2017[3].CWWright,etal.Invitroantiplasmodial,antiamoebic,andcytotoxicactivitiesofsomemonomericisoquinolinealkaloids.JNatProd.2000Dec;63(12):1638-40.McePdfHeightCaution:Producthasnotbeenfullyv