Usmarapride-free-base-SUVN-D4010-free-base-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEUsmarapridefreebaseCat.No.:HY-116565ACASNo.:1428862-32-1Synonyms:SUVN-D4010freebase分?式:C??H??N?O?分?量:383.49作?靶點(diǎn):5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥100mg/mL(260.76mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.6076mL13.0381mL26.0763mL5mM0.5215mL2.6076mL5.2153mL10mM0.2608mL1.3038mL2.6076mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(6.52mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.52mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.52mM);ClearsolutionBIOLOGICALACTIVITY?物活性Usmarapride(SUVN-D4010)freebase?種有效的、具有選擇性、?服活性和可透過(guò)?腦屏障的5-HT4受體部分激動(dòng)劑(EC50=nM)。Usmarapride(SUVN-D4010)freebase可?于阿爾茨海默病相關(guān)認(rèn)知缺陷的研究[1]。IC50&Target5-HT4Receptor44nM(EC50)體內(nèi)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