| Identification | Back Directory | [Name]
JNJ-1250132 | [CAS]
240805-96-3 | [Synonyms]
JNJ-1250132
19-Norpregna-4,9-diene-3,20-dione, 17-(acetyloxy)-11-[4-(1-piperidinyl)phenyl]-, (11β)- | [Molecular Formula]
C33H41NO4 | [MOL File]
240805-96-3.mol | [Molecular Weight]
515.69 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
JNJ-1250132 (10 mg/kg, oral, for seven days) inhibits Dexamethasone (HY-14648)-induced involution[1]. | [References]
[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. DOI:10.1016/j.steroids.2006.02.002 |
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