Zatolmilast-BPN14770-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEZatolmilastCat.No.:HY-117571CASNo.:1606974-33-7Synonyms:BPN14770分⼦式:C₂₁H₁₅ClF₃NO₂分⼦量:405.8作⽤靶点:Phosphodiesterase(PDE)作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:260mg/mL(640.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4643mL12.3213mL24.6427mL5mM0.4929mL2.4643mL4.9285mL10mM0.2464mL1.2321mL2.4643mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.17mg/mL(5.35mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(5.35mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Zatolmilast(BPN14770)⼀种选择性磷酸⼆酯酶4D(PDE4D)变构抑制剂，对于PDE4D7与PDE4D3的IC50值分别为7.8nM和7.4nM[1]。IC50&TargetPDE4D3PDE4D77.4nM(IC50)7.8nM(IC50)体内研究ZatolmilastincreasesbraincAMP,increasesphosphorylationofCREBandincreasesproductionofbrain-derivedneurotrophicfactor(BDNF)inhippocampus[1].Zatolmilast(0.1-30mg/kg;p.o.;24hours)providescognitivebenefitinthemousenovelobjectrecognition(NOR)atdosesabove0.3mg/kg[2].AnimalModel:C57Bl6mice[2]Dosage:0.1,0.3,1,3,10,30mg/kgAdministration:p.o.;24ꢀhoursResult:Significantlyimprovednovelobjectdiscriminationatdosesabove0.3mg/kg.REFERENCES[1].RicciarelliR,etal.Memory-enhancingeffectsofGEBR-32a,anewPDE4DinhibitorholdingpromiseforthetreatmentofAlzheimer'sdisease.SciRep.2017Apr12;7:46320.[2].GurneyME,etal.DesignandSynthesisofSelectivePhosphodiesterase4D(PDE4D)AllostericInhibitorsfortheTreatmentofFragileXSyndromeandOtherBrainDisorders.JMedChem.2019May23;62(10):4884-4901.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseon