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

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEUsmaraprideCat.No.:HY-116565CASNo.:1428862-33-2Synonyms:SUVN-D4010分?式:C??H??N?O?分?量:473.52作?靶點:5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:33.33mg/mL(70.39mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1118mL10.5592mL21.1184mL5mM0.4224mL2.1118mL4.2237mL10mM0.2112mL1.0559mL2.1118mL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(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?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：(為保證實驗結(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)實驗的?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%salineSolubility:2.5mg/mL(5.28mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.28mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.28mM);ClearsolutionBIOLOGICALACTIVITY?物活性Usmarapride(SUVN-D4010)?種有效的、具有選擇性、?服活性和可透過?腦屏障的5-HT4受體部分激動劑(EC50=nM)。Usmarapride(SUVN-D4010)可?于阿爾茨海默病相關(guān)認知缺陷的研究[1]。IC50&Target5-HT4Receptor44nM(EC50)體內(nèi)研究Usmarapride(SUVN-D4010)(1-3mg/kg;p.o.;MaleWistarrats10-12weeksold)attenuatesthelong-termmemorydeficitsinobjectrecognitiontest(ORT)[1].Usmarapride(1,3,and10mg/kg;p.o.)significantlyreversesthescopolamine-inducedamnesia[1].Usmaraprideshowsastatisticallysignificanteffectat3.0mg/kgonbothexplorationtimeandrecognitionindex[1].Usmarapride(SUVN-D4010)showsgoodoralexposures,goodbioavailability,andgoodbrainexposuresinrats[1].PharmacokineticofUsmaraprideinRats[1](3.0mg/kgforp.o.dosing;1.0mg/kgfori.v.)F%Cmax(ng/mL)AUC(ng·hr/mL)t1/2(h)Vdss(L/kg)CL(mLg/min/kg)343607091.78.076REFERENCES[1].Nirogi,Ramakrishna;Mohammed,AbdulRasheed;Yarlgadda,Suresh;Ravella,SrinivasaRao;Shinde,AnilKarbhari;Kambhampati,Ramasastri;Roayalley,PraveenKumar;Jayarajan,Pradeep;Bhyrapuneni,Gopinadh;Patnala,SriramachandraMurthy;etal.PreparatioMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre