S-Amisulpride-Esamisulpride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE(S)-AmisulprideCat.No.:HY-126068CASNo.:71675-92-8Synonyms:Esamisulpride;SEP-4199分⼦式:C₁₇H₂₇N₃O₄S分⼦量:369.48作⽤靶点:DopamineReceptor;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(270.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7065mL13.5325mL27.0651mL5mM0.5413mL2.7065mL5.4130mL10mM0.2707mL1.3533mL2.7065mL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:≥2.5mg/mL(6.77mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.77mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.77mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性(S)-Amisulpride(Esamisulpride)⼀种有效的多巴胺D2/D3受体拮抗剂。(S)-Amisulpride5-HT7受体的拮抗剂，KI值为900nM。(S)-Amisulpride具有抗精神和抗抑郁作⽤。IC50&TargetD2ReceptorD3Receptor5-HT7Receptor900nM(Ki)体外研究(S)-Amisulpride(Esamisulpride)displayshighaffinitybindingatbothD2andD3receptorsandisapproximatelytwiceaspotentasracamisulprideand20–50timesmorepotentthan(R)-amisulprideatthesereceptors[2]体内研究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