WAY-181187-SAX-187-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEWAY-181187Cat.No.:HY-14340CASNo.:554403-49-5Synonyms:SAX-187分?式:C??H??ClN?O?S?分?量:380.87作?靶點(diǎn):5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(262.56mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.6256mL13.1278mL26.2557mL5mM0.5251mL2.6256mL5.2511mL10mM0.2626mL1.3128mL2.6256mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(6.56mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(6.56mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.56mM);ClearsolutionBIOLOGICALACTIVITY?物活性WAY-181187(SAX-187)?種有效的選擇性5-HT6受體激動(dòng)劑，Ki為2.2nM，EC50為6.6nM[1]。WAY181187介導(dǎo)5-HT6受體依賴性信號(hào)通路，如cAMP，F(xiàn)yn和ERK1/2激酶，作為特異性激動(dòng)劑[1]。IC50&Target5-HT6Receptor5-HT6Receptor2.2nM(Ki)6.6nM(EC50)體外研究WAY181187(1and10μM)increasesactivationofERK1/2.WAY181187alsoincreasesFynkinaseactivity[2].WesternBlotAnalysis[2]CellLine:HEK/HA-5-HT6receptorcellsConcentration:1and10μMIncubationTime:Pretreatment5minutesResult:IncreasedactivationofERK1/2bothat1and10μMconcentrations.體內(nèi)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?邊的抑制劑?師www.MedChemENeuropsychopharmacology.2008May;33(6):1323-35.[2].TeresaRiccioni,etal.ST1936StimulatescAMP,Ca2+,ERK1/2andFynKinaseThroughaFullActivationofClonedHuman5-HT6Receptors.EurJPharmacol.2011Jul1;661(1-3):8-14.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap