Bioactivity | 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]. |
Invitro | JNJ-1250132 和 Mifepristone (HY-13683) 可抑制 R5020 (HY-119384) 刺激的细胞增殖,具有相似的半最大抑制浓度 (IC50 分别为 0.19 nM 和 0.17 nM)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> JNJ-1250132 相关抗体: |
In Vivo | JNJ-1250132 (10 mg/kg,口服,七天)可抑制 Dexamethasone (HY-14648) 诱导的退化[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS | 240805-96-3 |
Formula | C33H41NO4 |
Molar Mass | 515.68 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |