Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELY393615Cat.No.:HY-135478CASNo.:325819-97-4Synonyms:NCC1048分?式:C??H??ClF?NO分?量:381.89作?靶點(diǎn):CalciumChannel;SodiumChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性LY393615(NCC1048)?種新型神經(jīng)元Ca2+(calciumchannel)和Na+通道(sodiumchannel)阻滯劑。LY393615有良好的腦滲透性，在腦缺?模型中具有神經(jīng)保護(hù)作??？?于神經(jīng)性疾病研究。IC50&TargetP/Q-typecalciumchannel4μM(IC50)體外研究LY393615(0-10μΜ)inhibitscalciumfluxinHEK293cellswithα1Aandα1BcalciumchannelsubunitswithIC50sof1.9μΜand5.2μΜ,andinhibitsP-typecalciumchannelsinisolatedPurkinjecellswithIC50of4.0μΜ[1].體內(nèi)研究LY393615(10or12.5or15mg/kg;i.p.,singledose)protectsagainsthypoxiahypoglycaemicinsultsinbrainslicesandalsoprovidedsignificantprotectionagainstischaemia-inducedhippocampaldamageingerbilglobalcerebralischaemiasup[1].LY393615(15mg/kg;i.p.,1mg/kg;i.v.;singledose)hasgoodbrainpenetrationwithT1/2sof2.04hours(i.v.)and2.5hours(i.p.)[1].andpharmacokineticstudiesdemonstratedthatthecompoundhadgoodbrainpenetrationwithahalf-lifeof2-2.5h[1].AnimalModel:Gerbilsglobalcerebralischaemia[1]Dosage:10,12.5or15mg/kgAdministration:Intraperitonealinjection(i.p.)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Protectedagainsthypoxiahypoglycaemicinsultsinbrainslicesandalsoprovidedsignificantprotectionagainstischaemia-inducedhippocampaldamageingerbilglobalcerebralischaemia.AnimalModel:Gerbils(Pharmacokineticassay)[1]Dosage:1.0or15mg/kgAdministration:Intraperitonealinjection(i.p.);Intravenousinjection(i.v.)Result:PharmacokineticparametersforLY393615inGerbils[1]RouteDose(mg/kg)T1/2(h)i.v.12.04i.p.152.5REFERENCES[1].O'NeillMJ,et.al.LY393615,anovelneuronalCa(2+)andNa(+)channelblockerwithneuroprotectiveeffectsinmodelsofinvitroandinvivocerebralischemia.BrainRes.2001Jan5;888(1):138-149.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly