JNJ-1250132  (Synonyms: RWJ-66826; RTI-6617-003)

JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC₅₀ of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC₅₀=0.50 nM) and the rat androgen receptor (AR) (IC₅₀=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC₅₀ >3000 nM)^[1].

JNJ-1250132 and Mifepristone (HY-13683) inhibits R5020 (HY-119384)-stimulated cell proliferation at similar half-maximal inhibitory concentrations (IC₅₀s of 0.19 nM and 0.17 nM, respectively)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ-1250132 (10 mg/kg, oral, for seven days) inhibits Dexamethasone (HY-14648)-induced involution^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

515.68

C₃₃H₄₁NO₄

240805-96-3

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Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Allan GF, et al. Molecular properties and preclinical pharmacology of JNJ-1250132, a steroidal progesterone receptor modulator that inhibits binding of the receptor to DNA in vitro. Steroids. 2006 Jul;71(7):578-84.  [Content Brief]