S-Amisulpride-Esamisulpride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE(S)-AmisulprideCat.No.:HY-126068CASNo.:71675-92-8Synonyms:Esamisulpride;SEP-4199分?式:C??H??N?O?S分?量:369.48作?靶點(diǎn):DopamineReceptor;5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?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(270.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7065mL13.5325mL27.0651mL5mM0.5413mL2.7065mL5.4130mL10mM0.2707mL1.3533mL2.7065mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(6.77mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.77mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.77mM);ClearsolutionBIOLOGICALACTIVITY?物活性(S)-Amisulpride(Esamisulpride)?種有效的多巴胺D2/D3受體拮抗劑。(S)-Amisulpride5-HT7受體的拮抗劑，KI值為900nM。(S)-Amisulpride具有抗精神和抗抑郁作?。IC50&TargetD2ReceptorD3Receptor5-HT7Receptor900nM(Ki)體外研究(S)-Amisulpride(Esamisulpride)displayshighaffinitybindingatbothD2andD3receptorsandisapproximatelytwiceaspotentasracamisulprideand20–50timesmorepotentthan(R)-amisulprideatthesereceptors[2]體內(nèi)研究The(S)-amisulpride(10mg/kg,s.c.)stimulusisrapidlyacquiredandwasshowntobedose-related,timedependent(effectivebetween30and120min)andstereoselectivemaleC57BL/6mice[1].REFERENCES[1].TimothyJDonahue,etal.(S)-amisulprideasadiscriminativestimulusinC57BL/6miceanditscomparisontothestimuluseffectsoftypicalandatypicalantipsychotics.EurJPharmacol.2014Jul5;734:15-22.[2].VincentGrattan,etal.AntipsychoticBenzamidesAmisulprideandLB-102DisplayPolypharmacyasRacemates,SEnantiomersEngageReceptorsD2andD,whileREnantiomersEngage5-HT.ACSOmega.2019Aug15;4(9):14151-14154.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch