Progesterone Receptor Antagonist

Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC₅₀s of 0.2 nM and 2.6 nM in in vitro assay.

Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.

PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a K_i of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo.

Mifepristone (Standard) is the analytical standard of Mifepristone. This product is intended for research and analytical applications. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC₅₀s of 0.2 nM and 2.6 nM in in vitro assay.

PR antagonist 1 (compound 8) is a selective progesterone receptor (PR) antagonist, and can be used for the research of a variety of progesterone-related diseases and disorders such as endometriosis and uterine fibroids.

Mifepristone-d₃ is the deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC₅₀s of 0.2 nM and 2.6 nM in in vitro assay.

Mifepristone-d₆ is deuterated labeled Mifepristone (HY-13683). Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC₅₀s of 0.2 nM and 2.6 nM in in vitro assay.

PF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC₅₀=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds to progesterone receptor (PR) with the binding IC₅₀ of 310 nM.

Mifepristone-¹³C,d₃ is the ¹³C- and deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC₅₀s of 0.2 nM and 2.6 nM in in vitro assay. Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

W-255348 is an effective non-steroidal progesterone receptor (PR) antagonist that acquires antagonist activity by binding to and subsequently blocking progesterone induced nuclear accumulation, phosphorylation, and PR promoter interactions. WAY-255348 can be used in the research of reproductive disorders or PR-positive breast cancer.

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).

Ulipristal acetate-d₆ is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.

Onapristone is a progesterone receptor antagonist, with K_ds of 11.6 nM and 11.90 nM for human endometrium and myometrium progesterone receptor in saturation analysis. Onapristone has antitumor activity.

Cymipristone (ZXH-951), a progesterone receptor antagonist, is used potentially for termination of intrauterine pregnancy.

ZK112993 is a potent progesterone receptor (PR) antagonist. ZK112993 significantly inhibits the growth of T61 human tumors in nude mice.

Lonaprisan (ZK 230211; BAY86 5044) is an antagonist for progesterone receptor, with IC₅₀ of 3.6 pM and 2.5 pM for PR-A and PR-B, respectively. Lonaprisan exhibits antiprogestagenic activity in rabbits, interrupts early pregnancy in rats, and exhibits antitumor efficacy against DMBA (HY-W011845)-induced mammary tumor. Lonaprisan reveals antiglucocorticoid and antiandrogenic effect.

CP8754 is an orally active, selective human progesterone receptor (hPR) antagonist that blocks progesterone-mediated signaling pathways. CP8754 competitively inhibits the binding of [³H]-progesterone to hPR. And in vitro, CP8754 inhibits progesterone-dependent exogenous luciferase and endogenous alkaline phosphatase expression; while in vivo, CP8754 inhibits rabbit endometrial transformation. CP8754 does not significantly bind to human glucocorticoid receptors (hGR), estrogen receptors (hER), or rat androgen receptors (rAR). CP8754 can be used in the study of progesterone-related diseases such as breast cancer, endometriosis, uterine fibroids, and meningioma, as well as hormone-dependent tumors.

PF 02367982 is a potent and select progesterone receptor (PR) antagonist with an IC₅₀ value of 47.3 nM. PF 02367982 has oral activity.

Telapristone is a Progesterone antagonist. Telapristone can be used in the study of uterine fibroids and endometriosis.

Ulipristal acetate (Standard) is the analytical standard of Ulipristal acetate. This product is intended for research and analytical applications. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.