MRE-269-ACT-333679-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMRE-269Cat.No.:HY-79593CASNo.:475085-57-5Synonyms:ACT-333679分⼦式:C₂₅H₂₉N₃O₃分⼦量:419.52作⽤靶点:ProstaglandinReceptor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:50mg/mL(119.18mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3837mL11.9184mL23.8368mL5mM0.4767mL2.3837mL4.7674mL10mM0.2384mL1.1918mL2.3837mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.5mg/mL(5.96mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(5.96mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.96mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性MRE-269selexipag的有效代谢物，同时为选择性的IP受体激动剂。IC50&TargetIPReceptor体外研究MRE-269inducesendothelium-independentvasodilationofratextralobarpulmonaryartery(EPA).MRE-269orotherIPreceptoragonistsincludingepoprostenol,iloprost,treprostinilandberaprostincreasecAMPlevelsinhPASMC[1].MRE-269inducesconcentration-dependentvasodilationinLPA(+),LPA(-),andSPA(-)[3].体内研究ThevasorelaxanteffectsofMRE-269onratsmallintralobarpulmonaryartery(SIPA)andEPAarethesame,whiletheotherIPreceptoragonistsinducelessvasodilationinSIPAthaninEPA[1].MRE-269producessubstantialrelaxationofratsmallpulmonaryartery,althoughitseffectsareonlysignificantathighconcentrationsofabove10μM(pEC50,4.98±0.22).Bycontrast,inratsmallpulmonaryveins,MRE-269onlyproducesminimalrelaxationoverthewholeconcentrationrange,withonlysignificantrelaxationoccurringatthetwohighestdosesofMRE-269of10and100μM[2].REFERENCES[1].FuchikamiC,etal.Acomparisonofvasodilationmodeamongselexipag(NS-304;[2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide]),itsactivemetaboliteMRE-269andvariousprostacyclinreceptoragonistsinrat,porcin[2].OrieNN,etal.Differentialactionsoftheprostacyclinanaloguestreprostinilandiloprostandtheselexipagmetabolite,MRE-269(ACT-333679)inratsmallpulmonaryarteriesandveins.ProstaglandinsOtherLipidMediat.2013Oct;106:1-7[3].KuwanoK,etal.Along-actingandhighlyselectiveprostacyclinreceptoragonistprodrug,2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide(NS-304),amelioratesratpulmonaryhypertensionwithuniquerelaxantresponsesMcePdfHeightCaution:Producthasnotbeenfullyvalidatedfor