Ralinepag-APD811-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERalinepagCat.No.:HY-16751CASNo.:1187856-49-0Synonyms:APD811分?式:C??H??ClNO?分?量:431.91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:≥100mg/mL(231.53mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3153mL11.5765mL23.1530mL5mM0.4631mL2.3153mL4.6306mL10mM0.2315mL1.1576mL2.3153mL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?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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.79mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.79mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.79mM);ClearsolutionBIOLOGICALACTIVITY?物活性Ralinepag?種有效的，可?服的，?前列腺素類prostacyclin(IP)receptor激動劑，對?和??的IP受體的EC50值分別為8.5nM和530nM，對?DP1受體的EC50值為850nM。IC50&TargethIPrIP8.5nM(EC50)530nM(EC50)體外研究Ralinepagisapotentnon-prostanoidprostacyclinreceptoragonist,withEC50sof8.5nM,530nMand850nMforhumanandratIPreceptorandhumanDP1receptor,respectively.Ralinepag(5c)haspotentreceptorbindingaffinityatprostaglandinreceptor,withKisof1.2nM,3nM,76nM,and256nMformonkey,human,rat,anddogIPreceptor(ligand,[3H]-iloprost),and2.6μM,9.6μM,610nM,143nM,and678nMforhumanDP1,EP1,EP2,EP3v6andEP4receptors(ligand,[3H]-PGE2),respectively.Moreover,RalinepagshowsnoeffectoncytochromeP450enzymes(IC50>50μMforCYPs1A2,2D6,3A42C8,2C9,and2C19)orhERGchannelfunctionalactivityinapatchclampassay(IC50>30μM).RalinepagalsoinhibitstheADP-inducedhumanplateletaggregation,withanIC50of38nM[1].體內(nèi)研究Ralinepag(30mg/kg,p.o.)markedlyreducesthemonocrotaline(MCT)-inducedincreaseinpulmonaryarterialpressureandpulmonaryvesselwallthicknessinrats[1].REFERENCES[1].TranTA,etal.Discoveryof2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate(Ralinepag):AnOrallyActiveProstacyclinReceptorAgonistfortheTreatmentofPulmonaryArterialHypertension.JMedChem.2017Feb9;6McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicati