LY393615-NCC1048-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELY393615Cat.No.:HY-135478CASNo.:325819-97-4Synonyms:NCC1048分⼦式:C₂₁H₂₆ClF₂NO分⼦量:381.89作⽤靶点:CalciumChannel;SodiumChannel作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性LY393615(NCC1048)⼀种新型神经元Ca2+(calciumchannel)和Na+通道(sodiumchannel)阻滞剂。LY393615有良好的脑渗透性，在脑缺⾎模型中具有神经保护作⽤。可⽤于神经性疾病研究。IC50&TargetP/Q-typecalciumchannel4μM(IC50)体外研究LY393615(0-10μΜ)inhibitscalciumfluxinHEK293cellswithα1Aandα1BcalciumchannelsubunitswithIC50sof1.9μΜand5.2μΜ,andinhibitsP-typecalciumchannelsinisolatedPurkinjecellswithIC50of4.0μΜ[1].体内研究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—您⾝边的抑制剂⼤师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