1. Signaling Pathways
  2. Vitamin D Related/Nuclear Receptor
  3. Progesterone Receptor

Progesterone Receptor

NR3C3

Progesterone receptor (PR) is a member of the steroid/thyroid hormone-retinoid receptor superfamily of ligand-activated nuclear transcription factors. Progesterone receptor plays a vital role in female reproductive tissue development, differentiation, and maintenance.

Progesterone receptor is able to bind to a large number and variety of ligands that elicit a broad range of transcriptional responses ranging from full agonism to full antagonism and numerous mixed profiles inbetween. Progesterone receptor, such as progesterone, induces conformation changes in PR ligand binding domain (LBD), thus mediates subsequent gene regulation cascades.

In humans, the biological response to progesterone is mediated by two distinct forms of the progesterone receptor (human PR-A and PR-B).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-167932
    Mifepristone methochloride
    Inhibitor
    Mifepristone (RU486) methochloride is a glucocorticoid antagonist that blocks peripheral glucocorticoid and progesterone receptors. Mifepristone methochloride has been shown to have minimal effects on intraocular pressure in treated rabbits. Mifepristone methochloride was developed as a water-soluble formulation to enhance ocular penetration of the drug.
    Mifepristone methochloride
  • HY-B0084S4
    Dienogest-13C,15N,d4
    Agonist
    Dienogest-13C,15N,d4 (STS 557-13C,15N,d4) is the 13C, 15N and deuterium labeled isotope of Dienogest (HY-B0084). Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia.
    Dienogest-<sup>13</sup>C,<sup>15</sup>N,d<sub>4</sub>
  • HY-17649
    EIDD-036
    EIDD-036, is the blood-brain barrier penetrant C-20 oxime of Progesterone (HY-N0437), that binds progesterone receptor (PR) with an IC50 of 171 nM. EIDD-036 is the active metabolite of EIDD-1723 (HY-125547). EIDD-036 exhibits promising challenges for rapid administration in acute trauma. EIDD-036 can be used for the study of traumatic brain injury (TBI).
    EIDD-036
  • HY-B0257AR
    Dydrogesterone (Standard)
    Agonist
    Dydrogesterone (Standard) is the analytical standard of Dydrogesterone. This product is intended for research and analytical applications. Dydrogesterone is a potent, orally active progestogen indicated in a wide variety of gynaecological conditions related to progesterone deficiency.
    Dydrogesterone (Standard)
  • HY-126762
    Fenprostalene
    Fenprostalene is an analog of Dinoprost (PGF2α) (HY-12956) that is used in veterinary medicine to induce corpus luteum regression and blood Progesterone (HY-N0437) levels reduction in dogs. Fenprostalene is potent in ameliorating pyometra and inducing abortion.
    Fenprostalene
  • HY-B0111S1
    Drospirenone-d4-1
    Agonist
    Drospirenone-d4-1 is deuterium labeled Drospirenone.
    Drospirenone-d<sub>4</sub>-1
  • HY-111614S
    Melengestrol acetate-d6
    Activator
    Melengestrol acetate-d6 is the deuterium labeled Melengestrol acetate. Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research.
    Melengestrol acetate-d<sub>6</sub>
  • HY-123163
    JNJ-1250132
    Antagonist
    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).
    JNJ-1250132
  • HY-B0257S
    Levonorgestrel-d8
    Agonist
    Levonorgestrel-d8 is the deuterium labeled Levonorgestrel. Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives. Levonorgestrel-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Levonorgestrel-d<sub>8</sub>
  • HY-16508S
    Ulipristal acetate-d6
    Antagonist
    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.
    Ulipristal acetate-d<sub>6</sub>
  • HY-106827
    Trimegestone
    Modulator
    Trimegestone (RU 27987) is an orally active, selective progestogen and PR ligand, with an IC50 of 7.6 nM for hPR, 4.4 nM for rabbit PR, and 3.3 nM for rat PR. Trimegestone induces Alkaline phosphatase activity. Trimegestone exhibits antiandrogenic activity (IC50 = 303 nM). Trimegestone can be used in research related to menopausal symptoms and osteoporosis.
    Trimegestone
  • HY-108979
    Medrogestone
    Medrogestone is an orally active Progestin. Medrogestone shows a marked local progestational effect. Medrogestone maintains pregnancy in ovariectomized rats. Medrogestone inhibits ovulation. Medrogestone prevents pregnancy. Medrogestone produces a significant reduction in the severity of benign prostatic hypertrophy.
    Medrogestone
  • HY-B0084S
    Dienogest-d4
    Agonist
    Dienogest-d4 is deuterium labeled Dienogest.
    Dienogest-d<sub>4</sub>
  • HY-125547
    EIDD-1723
    EIDD-1723 is a Progesterone (HY-N0437) analogues, that binds progesterone receptor (PR) with an IC50 of 2.25 μM. EIDD-1723 is the prodrug of EIDD-036 (HY-17649). EIDD-1723 may exert its neuroprotective effects not solely through progesterone receptor (PR)-dependent pathways but also via non-genomic mechanisms, such as modulation of inflammatory responses and oxidative stress. EIDD-1723 can be used for the study of traumatic brain injury (TBI).
    EIDD-1723
  • HY-186011
    CPAG-1
    Activator
    CPAG-1 is a small-molecule activator of progesterone receptor membrane component 2 (PGRMC2). CPAG-1 can enhance mitochondrial heme delivery to the nucleus mediated by PGRMC2 and activate genes related to heat production in brown adipose tissue (BAT), such as Ucp1 and Pgc-1α, and reduce lipid accumulation in BAT. CPAG-1 reduce fasting blood sugar and insulin levels, and improve glucose tolerance and insulin sensitivity. CPAG-1 can be used for research of type 2 diabetes.
    CPAG-1
  • HY-106389
    Onapristone
    Antagonist
    Onapristone is a progesterone receptor antagonist, with Kds of 11.6 nM and 11.90 nM for human endometrium and myometrium progesterone receptor in saturation analysis. Onapristone has antitumor activity.
    Onapristone
  • HY-W746582
    Norethindrone-d7
    Norethindrone-d7 (Norethisterone-d7) is the deuterium labeled Norethindrone (HY-B0554). Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
    Norethindrone-d<sub>7</sub>
  • HY-105634
    Nomegestrol
    Agonist
    Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
    Nomegestrol
  • HY-B1095R
    Chlormadinone acetate (Standard)
    Agonist
    Chlormadinone acetate (Standard) is the analytical standard of Chlormadinone acetate (HY-B1095). This product is intended for research and analytical applications. Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABAA receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders.
    Chlormadinone acetate (Standard)
  • HY-B0084S1
    Dienogest-d5
    Agonist
    Dienogest-d5 is deuterium labeled Dienogest.
    Dienogest-d<sub>5</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity