Usmarapride-free-base-SUVN-D4010-free-base-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEUsmarapridefreebaseCat.No.:HY-116565ACASNo.:1428862-32-1Synonyms:SUVN-D4010freebase分⼦式:C₂₁H₂₉N₅O₂分⼦量:383.49作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(260.76mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6076mL13.0381mL26.0763mL5mM0.5215mL2.6076mL5.2153mL10mM0.2608mL1.3038mL2.6076mL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(6.52mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.52mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.52mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Usmarapride(SUVN-D4010)freebase⼀种有效的、具有选择性、⼝服活性和可透过⾎脑屏障的5-HT4受体部分激动剂(EC50=nM)。Usmarapride(SUVN-D4010)freebase可⽤于阿尔茨海默病相关认知缺陷的研究[1]。IC50&Target5-HT4Receptor44nM(EC50)体内研究Usmarapride(SUVN-D4010)(1-3mg/kg;p.o.;MaleWistarrats10-12weeksold)freebaseattenuatesthelong-termmemorydeficitsinobjectrecognitiontest(ORT)[1].Usmarapride(1,3,and10mg/kg;p.o.)freebasesignificantlyreversesthescopolamine-inducedamnesia[1].Usmarapridefreebaseshowsastatisticallysignificanteffectat3.0mg/kgonbothexplorationtimeandrecognitionindex[1].Usmarapride(SUVN-D4010)freebaseshowsgoodoralexposures,goodbioavailability,andgoodbrainexposuresinrats[1].REFERENCES[1].NirogiR,etal.DiscoveryandPreclinicalCharacterizationofUsmarapride(SUVN-D4010):APotent,Selective5-HT4ReceptorPartialAgonistfortheTreatmentofCognitiveDeficitsAssociatedwithAlzheimer'sDisease.JMedChem.2021;64(15):10641-10665.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse