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

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEUsmaraprideCat.No.:HY-116565CASNo.:1428862-33-2Synonyms:SUVN-D4010分⼦式:C₂₃H₃₁N₅O₆分⼦量:473.52作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:33.33mg/mL(70.39mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1118mL10.5592mL21.1184mL5mM0.4224mL2.1118mL4.2237mL10mM0.2112mL1.0559mL2.1118mL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(sealedstorage,awayfrommoisture)。-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%salineSolubility:2.5mg/mL(5.28mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.28mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.28mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Usmarapride(SUVN-D4010)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)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)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