XPC-6444-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEXPC-6444Cat.No.:HY-128772CASNo.:2230144-21-3分⼦式:C₂₂H₂₅F₃N₄O₂S₂分⼦量:498.58作⽤靶点:SodiumChannel作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(250.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0057mL10.0285mL20.0570mL5mM0.4011mL2.0057mL4.0114mL10mM0.2006mL1.0028mL2.0057mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.17mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.17mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性XPC-6444⼀种⾼效的，亚型选择性的，CNS-渗透性的NaV1.6抑制剂(对hNaV1.6的IC50=41nM)。XPC-6444也有效阻断了NaV1.2(IC50=125nM)。XPC-6444具有抗惊厥活性。IC50&TargetIC50:41nM(hNaV1.6),125nM(hNaV1.2)[1]体外研究XPC-6444showshighselectivityoverNaV1.1andNaV1.5[1].体内研究XPC-6444exhibitsgoodmetabolicstabilityinhumanlivermicrosomesandhepatocytes,andlowpotentialforMDR1mediatedefflux[1].REFERENCES[1].FockenT,etal.IdentificationofCNS-PenetrantArylSulfonamidesasIsoform-SelectiveNaV1.6InhibitorswithEfficacyinMouseModelsofEpilepsy.JMedChem.2019Oct3.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021