Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEONO-7300243Cat.No.:HY-100882CASNo.:638132-34-0分?式:C??H??NO?分?量:461.55作?靶點(diǎn):LPLReceptor作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(216.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1666mL10.8331mL21.6661mL5mM0.4333mL2.1666mL4.3332mL10mM0.2167mL1.0833mL2.1666mL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。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?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:≥3mg/mL(6.50mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥3mg/mL(6.50mM);ClearsolutionBIOLOGICALACTIVITY?物活性O(shè)NO-7300243?種新型有效的溶?磷脂酸受體1(LPA1)拮抗劑，IC50為0.16μM。IC50&TargetIC50:0.19-0.13μM(LPA1)[1]體外研究ONO-7300243showsmodestinvitroactivity(IC50=0.16μM).ONO-7300243exhibitsalmostidenticallevelsofantagonistactivityinvitro[1].體內(nèi)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