MRE-269-ACT-333679-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMRE-269Cat.No.:HY-79593CASNo.:475085-57-5Synonyms:ACT-333679分?式:C??H??N?O?分?量:419.52作?靶點:ProstaglandinReceptor作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(119.18mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3837mL11.9184mL23.8368mL5mM0.4767mL2.3837mL4.7674mL10mM0.2384mL1.1918mL2.3837mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?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：(為保證實驗結(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)實驗的?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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.5mg/mL(5.96mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(5.96mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.96mM);ClearsolutionBIOLOGICALACTIVITY?物活性MRE-269selexipag的有效代謝物，同時為選擇性的IP受體激動劑。IC50&TargetIPReceptor體外研究MRE-269inducesendothelium-independentvasodilationofratextralobarpulmonaryartery(EPA).MRE-269orotherIPreceptoragonistsincludingepoprostenol,iloprost,treprostinilandberaprostincreasecAMPlevelsinhPASMC[1].MRE-269inducesconcentration-dependentvasodilationinLPA(+),LPA(-),andSPA(-)[3].體內(nèi)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