JNJ-1250132-RWJ-66826-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEJNJ-1250132Cat.No.:HY-123163CASNo.:240805-96-3Synonyms:RWJ-66826;RTI-6617-003分?式:C??H??NO?分?量:515.68作?靶點(diǎn):ProgesteroneReceptor;GlucocorticoidReceptor;AndrogenReceptor;EstrogenReceptor/ERR作?通路:VitaminDRelated/NuclearReceptor;Immunology/Inflammation儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性JNJ-1250132(RWJ-66826)?種?服有效的類醇孕酮受體(PR)拮抗劑，其IC50為1.3nM。JNJ-1250132可在體外抑制受體與DNA的結(jié)合。JNJ-1250132?種強(qiáng)效的競(jìng)爭(zhēng)性抑制劑，可與?類糖?質(zhì)激素受體(GR)(IC50=0.50nM)和??雄激素受體(AR)(IC50=5.6nM)結(jié)合，并且與?類雌激素受體(ER)(IC50>3000nM)結(jié)合的弱抑制劑。體外研究JNJ-1250132andMifepristone(HY-13683)inhibitsR5020(HY-119384)-stimulatedcellproliferationatsimilarhalf-maximalinhibitoryconcentrations(IC50sof0.19nMand0.17nM,respectively)[1].體內(nèi)研究JNJ-1250132(10mg/kg,oral,forsevendays)inhibitsDexamethasone(HY-14648)-inducedinvolution[1].REFERENCES[1].AllanGF,etal.MolecularpropertiesandpreclinicalpharmacologyofJNJ-1250132,asteroidalprogesteronereceptormodulatorthatinhibitsbindingofthereceptortoDNAinvitro.Steroids.2006Jul;71(7):578-84.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792ax:021-5370