WAY-181187-SAX-187-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEWAY-181187Cat.No.:HY-14340CASNo.:554403-49-5Synonyms:SAX-187分⼦式:C₁₅H₁₃ClN₄O₂S₂分⼦量:380.87作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(262.56mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6256mL13.1278mL26.2557mL5mM0.5251mL2.6256mL5.2511mL10mM0.2626mL1.3128mL2.6256mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.56mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(6.56mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.56mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性WAY-181187(SAX-187)⼀种有效的选择性5-HT6受体激动剂，Ki为2.2nM，EC50为6.6nM[1]。WAY181187介导5-HT6受体依赖性信号通路，如cAMP，Fyn和ERK1/2激酶，作为特异性激动剂[1]。IC50&Target5-HT6Receptor5-HT6Receptor2.2nM(Ki)6.6nM(EC50)体外研究WAY181187(1and10μM)increasesactivationofERK1/2.WAY181187alsoincreasesFynkinaseactivity[2].WesternBlotAnalysis[2]CellLine:HEK/HA-5-HT6receptorcellsConcentration:1and10μMIncubationTime:Pretreatment5minutesResult:IncreasedactivationofERK1/2bothat1and10μMconcentrations.体内研究AcuteadministrationofWAY-181187(3-30mg/kg,s.c.)significantlyincreasesextracellularGABAconcentrationswithoutalteringthelevelsofglutamateornorepinephrineintheratfrontalcortex.Additionally,WAY-181187(30mg/kg,s.c.)producesmodestyetsignificantdecreasesincorticaldopamineand5-HTlevels[1].AnimalModel:AdultmaleSprague-Dawleyratsweighing280–350g[1]Dosage:3,10,or30mg/kgAdministration:Acutedministeredbys.c.Result:SignificantlyincreasedextracellularGABAconcentrationswithoutalteringthelevelsofglutamateornorepinephrine.REFERENCES[1].LeeESchechter,etal.NeuropharmacologicalProfileofNovelandSelective5-HT6ReceptorAgonists:WAY-181187andWAY-208466.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemENeuropsychopharmacology.2008May;33(6):1323-35.[2].TeresaRiccioni,etal.ST1936StimulatescAMP,Ca2+,ERK1/2andFynKinaseThroughaFullActivationofClonedHuman5-HT6Receptors.EurJPharmacol.2011Jul1;661(1-3):8-14.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap