CP8754 is a selective antagonist of the human progesterone receptor (hPR), acting primarily by competitively inhibiting the binding of [3H]-progesterone. This compound effectively impedes progesterone-mediated signaling, as evidenced by its ability to inhibit both exogenous luciferase and endogenous alkaline phosphatase expression in vitro, and to suppress rabbit endometrial transformation in vivo. CP8754 exhibits minimal binding affinity for human glucocorticoid receptors, estrogen receptors, and rat androgen receptors, making it a valuable tool for investigating progesterone-related diseases, including breast cancer, endometriosis, uterine fibroids, and hormone-dependent tumors.
CP8754 is a selective antagonist of the human progesterone receptor (hPR), acting primarily by competitively inhibiting the binding of [3H]-progesterone. This compound effectively impedes progesterone-mediated signaling, as evidenced by its ability to inhibit both exogenous luciferase and endogenous alkaline phosphatase expression in vitro, and to suppress rabbit endometrial transformation in vivo. CP8754 exhibits minimal binding affinity for human glucocorticoid receptors, estrogen receptors, and rat androgen receptors, making it a valuable tool for investigating progesterone-related diseases, including breast cancer, endometriosis, uterine fibroids, and hormone-dependent tumors.
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