Relenopride-hydrochloride-YKP10811-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERelenopridehydrochlorideCat.No.:HY-16729ACASNo.:1221416-42-7Synonyms:YKP10811hydrochloride分⼦式:C₂₄H₃₁Cl₂FN₄O₄分⼦量:529.43作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性数据体外实验DMSO:110mg/mL(207.77mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8888mL9.4441mL18.8882mL5mM0.3778mL1.8888mL3.7776mL10mM0.1889mL0.9444mL1.8888mL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(protectfromlight,storedundernitrogen)。-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:≥2.75mg/mL(5.19mM);Clearsolution1/2MasterofBioactiveMolecules—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:≥2.75mg/mL(5.19mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(5.19mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Relenopride(YKP10811)hydrochloride⼀种特异性和选择性的5-HT4受体激动剂(Ki=4.96nM)。与5-HT4相⽐，Relenopridehydrochloride对5-HT2A(Ki=600nM)和5-HT2B(Ki=31nM)受体的亲和⼒分别低120倍和6倍。Relenopridehydrochloride增加胃肠运动。IC50&Target5-HT4Receptor5-HT2AReceptor5-HT2BReceptor5-HT2BReceptor4.96nM(Ki)600nM(Ki)31nM(Ki)2.1μM(IC50)体外研究Relenopridehydrochloridedonotshowanysignificantoff-targetbindingtoanyotherreceptors,enzymes,orserotonin-receptorsubtypesat1μM,exceptforbindingtothe5-HT2Areceptorandthe5-HT2Breceptor.Relenopridehydrochlorideshowsantagonistactivityatthe5-HT2BreceptorwithanIC50of2.1μMandnosignificantactivityatthe5-HT2Areceptorupto10μM.Relenopridehydrochlorideshowsnoactivityagainstserotonin-receptorsubtypes5-HT1B,5-HT1D,or5-HT2Aat1nMto10μM,orforserotonin-receptorsubtype5-HT7at10nMto30μM[1].REFERENCES[1].ShinA,etal.Arandomizedtrialof5-hydroxytryptamine4-receptoragonist,YKP10811,oncolonictransitandbowelfunctioninfunctionalconstipation.ClinGastroenterolHepatol.2015;13(4):701-8.e1.[2].YinJ,etal.Prokineticeffectsofanew5-HT4agonist,YKP10811,ongastricmotilityindogs.JGastroenterolHepatol.2017;32(3):625-630.[3].GiletM,etal.Influenceofanew5-HT4receptorpartialagonist,YKP10811,onvisceralhypersensitivityinratstriggeredbystressandinflammation.NeurogastroenterolMotil.2014;26(12):1761-1770.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical