Osilodrostat-phosphate-LCI699-phosphate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEOsilodrostatphosphateCat.No.:HY-16276ACASNo.:1315449-72-9Synonyms:LCI699phosphate分?式:C??H??FN?O?P分?量:325.23作?靶點(diǎn):MineralocorticoidReceptor作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:≥200mg/mL(614.95mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.0747mL15.3737mL30.7475mL5mM0.6149mL3.0747mL6.1495mL10mM0.3075mL1.5374mL3.0747mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性O(shè)silodrostat(LCI699)phosphate?種?服有效的11β-羥化酶(CYP11B1)抑制劑，其IC50值為35nM。Osilodrostatphosphate?種?服有效的醛酮合成酶(CYP11B2)抑制劑，抑制?醛酮合成酶和??醛固酮合成酶的IC50分別為0.7nM和160nM。Osilodrostatphosphate抑制醛酮和?質(zhì)酮的合成。Osilodrostatphosphate具有降低?壓的能?。Osilodrostatphosphate可?于庫(kù)欣綜合征(CS)的研究。1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIC50&TargetIC50:35nM(CYP11B1),0.7nM(humanaldosteronesynthase),and160nM(rataldosteronesynthase)[1][2]體外研究Osilodrostat(LCI699;0.01-10μM;HAC15cells,17primaryhumanadrenocorticalcellcultures,andpituitaryadenomacells)phosphateinhibitscortisolandaldosterone.Osilodrostatresultsininhibitionofcorticosterone,11-deoxycortisolaccumulation,andmodesteffectsonadrenalandrogens[2].體內(nèi)研究Osilodrostat(LCI699;0.1-100mg/kg;p.o.;once)phosphateinhibitsaldosteroneandcorticosteronesynthesisinAng-II-andACTH-stimulatedSpragueDawleyrats[1].Osilodrostat(LCI699;3-100mg/kg;p.o.;daily,for52weeks)phosphatereducesmeanarterialpressureandprolongssurvivalindTGrats[1].AnimalModel:MaleAng-II-andACTH-stimulatedSpragueDawleyrats[1]Dosage:0.1,0.3,1and3mg/kg(Ang-II-stimulatedrats)and1,3,10,30and100mg/kg(ACTH-stimulatedrats)Administration:Oraladministration;onceResult:InhibitedtheincreaseinplasmaaldosteroneconcentrationsstimulatedbyAngIIorACTHinadose-dependentmanner.AnimalModel:dTGrats[1]Dosage:3,10,30and100mg/kgAdministration:Oraladministration;daily,for52weeksResult:IncreasedfractionalLV(systolicanddiastolic)shortening,normalizedLVisovolumicrelaxationtimetoRR(IVRT/RR)ratioandmyocardialcellsizeandreducedLVweightinadose-dependentmanner.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ActaPharmSinB.21September2021.?BMCMed.2021Sep8;19(1):204.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MénardJ,et,al.Aldosteronesynthaseinhibition:cardiorenalprotectioninanimaldiseasemodelsandtranslationofhormonaleffectstohumansubjects.JTranslMed.2014Dec10;12:340.[2].CreemersSG,et,al.OsilodrostatIsaPotentialNovelSteroidogenesisInhibitorfortheTreatmentofCushingSyndrome:AnInVitroStudy.JClinEndocrinolMetab.2019Aug1;104(8):3437-3449.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[3].LiL,et,al.Osilodrostat(LCI699),apotent11β-hydroxylaseinhibitor,administeredincombinationwiththemultireceptor-targetedsomatostatinanalogpasireotide:A13-weekstudyinrats.ToxicolApplPharmacol.2015Aug1;286(3):224-33.McePdfHeightCaution:Producthasnotbeen