ONO-7300243-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEONO-7300243Cat.No.:HY-100882CASNo.:638132-34-0分⼦式:C₂₈H₃₁NO₅分⼦量:461.55作⽤靶点:LPLReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(216.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1666mL10.8331mL21.6661mL5mM0.4333mL2.1666mL4.3332mL10mM0.2167mL1.0833mL2.1666mL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。-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:≥3mg/mL(6.50mM);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%cornoilSolubility:≥3mg/mL(6.50mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ONO-7300243⼀种新型有效的溶⾎磷脂酸受体1(LPA1)拮抗剂，IC50为0.16μM。IC50&TargetIC50:0.19-0.13μM(LPA1)[1]体外研究ONO-7300243showsmodestinvitroactivity(IC50=0.16μM).ONO-7300243exhibitsalmostidenticallevelsofantagonistactivityinvitro[1].体内研究ONO-7300243showsgoodefficacyinvivo.Theoraldosingof17aat30mg/kgleadstoreducedintraurethralpressureinrats.ONO-7300243showsstrongeeffectsinvivo(88%inhibitionat10mg/kgi.d.,62%inhibitionat3mg/kgi.d.)comparedwithcompound12g.TheresultsrevealthatONO-7300243showsgoodmembranepermeabilityandgoodmetabolicstabilityagainstratlivermicrosomes(MS).ONO-7300243exhibitsgoodselectivitytowardsLPAloverLPA2,mostlikelybecauselowmolecularweightandlowlipophilicityleadtoreducedcompoundpromiscuityandincreasedselectivity.ONO-7300243inhibitstheLPA-inducedIUPincreaseinadosedependentmanner(ID50=11.6mg/kgp.o.)upto1hafterdosing.Significanteffectsareobservedat10and30mg/kg(p[1].PROTOCOLAnimalRats[1]Administration[1]TheoraladministrationofONO-7300243(30mg/kg,p.o.)isinvestigatedtodetermineitseffectonratIUP.ONO-7300243isstudiedinanLPA-inducedratintraurethralpressure(IUP)model.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].TerakadoM,etal.DiscoveryofONO-7300243fromaNovelClassofLysophosphatidicAcidReceptor1Antagonists:FromHittoLead.ACSMedChemLett.2016Aug19;7(10):913-918.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication