ONO-8711-dicyclohexylamine-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEONO-8711dicyclohexylamineCat.No.:HY-12182A分⼦式:C₃₄H₅₃ClN₂O₄S分⼦量:621.31作⽤靶点:ProstaglandinReceptor作⽤通路:GPCR/GProtein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:50mg/mL(80.48mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6095mL8.0475mL16.0950mL5mM0.3219mL1.6095mL3.2190mL10mM0.1610mL0.8048mL1.6095mL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。BIOLOGICALACTIVITY⽣物活性ONO-8711dicyclohexylamine⼀种有效的选择性竞争性EP1拮抗剂，对⼈和⼩⿏EP1的Ki值分别为0.6nM和1.7nM。ONO-8711dicyclohexylamine有效降低结肠癌、乳腺癌和⼝腔癌⼩⿏模型的肿瘤发⽣率。IC50&TargetKi:0.6nM(humanEP1),1.7nM(mouseEP1)[1]体外研究ONO-8711(10and30μM;30min)blocksthecontractionsinducedbysulprostoneinhumanpulmonaryveinsinanon-competitivemanner[2].ONO-8711inhibitsPGE2-inducedincreaseincytosolicCa2+concentrationwithIC50sof0.21μM,0.05μM,1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEand0.22μMforthemouse,human,andratreceptors,respectively[3].体内研究ONO-8711(400or800p.p.m.;p.o.;for20weeks)suppressescancerincidenceanddelaysoccurrenceofbreasttumors[3].AnimalModel:FemaleSprague-Dawleyrats(inducedbreastcancerbygavageof85mg/kgPhIP(HY-118716)4timesfor2weeks)Dosage:400or800p.p.m.Administration:p.o.;for20weeksResult:Didnotinduceanysymptomsoftoxicityat800p.p.m..Delayedoccurrenceofbreasttumorsfor2or4weeksat400or800p.p.m.,respectively.Significantlysuppressedcancerincidencecomparedwiththecontroldietgroupat800p.p.m.(56%versus79%,P<0.05).REFERENCES[1].WatanabeK,etal.RoleoftheprostaglandinEreceptorsubtypeEP1incoloncarcinogenesis.CancerRes.1999Oct15;59(20):5093-6.[2].NorelX,etal.VasoconstrictioninducedbyactivationofEP1andEP3receptorsinhumanlung:effectsofONO-AE-248,ONO-DI-004,ONO-8711orONO-8713.ProstaglandinsOtherLipidMediat.2004Oct;74(1-4):101-12.[3].KawamoriT,etal.ChemopreventiveeffectsofONO-8711,aselectiveprostaglandinEreceptorEP(1)antagonist,onbreastcancerdevelopment.Carcinogenesis.2001Dec;22(12):2001-4.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre