Relenopride-hydrochloride-YKP10811-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERelenopridehydrochlorideCat.No.:HY-16729ACASNo.:1221416-42-7Synonyms:YKP10811hydrochloride分?式:C??H??Cl?FN?O?分?量:529.43作?靶點(diǎn):5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:110mg/mL(207.77mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8888mL9.4441mL18.8882mL5mM0.3778mL1.8888mL3.7776mL10mM0.1889mL0.9444mL1.8888mL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(protectfromlight,storedundernitrogen)。-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(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)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(shí)驗(yàn)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(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:≥2.75mg/mL(5.19mM);Clearsolution1/2MasterofBioactiveMolecules—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:≥2.75mg/mL(5.19mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(5.19mM);ClearsolutionBIOLOGICALACTIVITY?物活性Relenopride(YKP10811)hydrochloride?種特異性和選擇性的5-HT4受體激動劑(Ki=4.96nM)。與5-HT4相?，Relenopridehydrochloride對5-HT2A(Ki=600nM)和5-HT2B(Ki=31nM)受體的親和?分別低120倍和6倍。Relenopridehydrochloride增加胃腸運(yùn)動。IC50&Target5-HT4Receptor5-HT2AReceptor5-HT2BReceptor5-HT2BReceptor4.96nM(Ki)600nM(Ki)31nM(Ki)2.1μM(IC50)體外研究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