Estrogen/progestogen Receptor

4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.

Allura Red AC (CI 16035) is a very important food azo dye used in the food, pharmaceutical, paper, cosmetic and textile industries.Allura Red AC promotes susceptibility to experimental colitis via mouse intestinal serotonin.

Medroxyprogesterone Acetate (Farlutin) is a synthetic progestin that is derived from 17-hydroxyprogesterone. It is a long-acting contraceptive that is effective both orally or by intramuscular injection and has also been used to treat breast and endometrial neoplasms.

Natamycin (Pimaricin) is a Polyene Antimicrobial.

Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist (IC50=9.4 nM) and an agonist of GPR30. Fulvestrant has antitumor activity, inhibiting cell proliferation and inducing apoptosis and autophagy.

Ulipristal acetate (CDB-2914) is an orally bioavailable, acetate salt of ulipristal, a selective progesterone receptor modulator with anti-progesterone activity. Ulipristal binds to the progesterone receptor (PR), thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system. As a result, this agent may suppress the growth of uterine leiomyomatosis. Furthermore, by inhibiting or delaying ovulation and effecting endometrial tissue, ulipristal can be used as an emergency contraception.

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

Chlorotrianisene (tri-p-anisylchloroethylene) is an orally bioavailable, highly lipophilic, synthetic triphenylethylene (TPE) derivative and selective estrogen receptor modulator (SERM), with predominantly estrogenic but also antiestrogenic activities.

Mifepristone (C-1073) is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist.

Ethisterone (17α-Ethynyltestosterone) is a progestogen hormone.

Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.

Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1 2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.

Levonorgestrel (D-Norgestrel) is a Progestin and Progestin-containing Intrauterine Device. The physiologic effect of levonorgestrel is by means of Inhibit Ovum Fertilization.

Zindoxifene (D 16726) is an anti-estrogenic compound with antitumor activity that can be used in studies of breast and prostate cancer.

Serba-2 is an agonist of benzopyran selective estrogen receptor beta.

Panomifene TFA（GYKl13504 TFA） is a small molecule antagonist of ERs with anticancer activity that can be used to study breast cancer and musculoskeletal diseases.

Cyclopenta[c][1]benzopyran-8-ol, 1,2,3,3a,4,9b-hexahydro-4-(4-hydroxyphenyl)-, (3aR,4S,9bS)-rel- is an estrogen receptor beta (ERβ) agonist.

SNG-1153 is a estrogen receptor ER-alpha36 modulator.

4,4'-Iminodiphenol (Leucoindophenol) is an inactive estrogen receptor ligand with a diphenylamine backbone.

OBHSA（Oxabicycloheptane sulfonamide） is a novel selective estrogen receptor depressant (SERD) that can be used to study breast cancer.

Indazole-Cl is a selective ERß agonist and a selective estrogen receptor modifier (SERM).

Estrogen receptor antagonist 8 acts as an estrogen receptor (ER) antagonist with anti-uterine activity and potential anti-tumorigenic activity and can be used to study ovarian dysfunction.

XR 5944 is an antitumor compound that targets DNA, is a topoisomerase inhibitor, inhibits ER activity, and can be used to study colon and lung cancer.

Erteberel (LY500307) is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.

LY88074 is a raloxifene analog in which the basic side chain has been removed. LY88074 is an agonist of ERβ (EC50 = 232 nM).This compound stimulates uterine cell proliferation.

Prinaberel (ERB-041) is an effective and selective ERβ agonist and >200-fold selective for ERβ.

ERRα antagonist-1 (ERR+/- antagonist-1) is a high-affinity, selective antagonist of the estrogen-related receptor α (ERRα). It effectively prevents the interaction of ERRα with both Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, displaying IC50 values of 170 nM and 180 nM, respectively. Notably, ERRα antagonist-1 does not interfere with the interactions involving ERRβ or ERRγ and the PGC-1α and PGC-1β coactivators. Furthermore, it does not affect the interaction between either ERα or ERβ and PGC-1α or SRC-1.

Liquiritigenin (4',7-Dihydroxyflavanone), a flavonoid aglycone from licorice, is a highly selective estrogen receptor β (ERβ) agonist.

DPN (Diarylpropionitrile) is an selective agonist of estrogen receptor β (ERβ) .

Epiandrosterone (EpiA) is a dehydroepiandrosterone metabolite and a precursor of testosterone and estradiol with hypolipidemic and anabolic property.

Medroxyprogesterone is used in the treatment of renal carcinoma. It is a synthetic progestational hormone used in veterinary practice as an estrus regulator.

Clomiphene citrate (NSC 35770) is a selective estrogen receptor modulator.

Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Ethynodiol diacetate (Ethynodiol acetate) is a synthetic progestational hormone used alone or in combination with estrogens as an oral contraceptive.

Bazedoxifene hydrochloride (TSE 424 hydrochloride) is an orally active, selective, and potent estrogen receptor modulator (SERM) that crosses the blood-brain barrier and is an inhibitor of IL-6 GP130 protein interactions with high affinity for ERα and ERβ. It has a high affinity for ERα and ERβ and can be used to study postmenopausal osteoporosis and vasodilator-related diseases.

Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM).

(E Z)-4-Hydroxytamoxifen (Afimoxifene) is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer.

Isopsoralenoside shows estrogen-like, osteoblastic proliferation accelerating, antitumor, and antibacterial effects.

Progesterone (Pregn-4-ene-3,20-dione) is the major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production.

Dienestrol (Restrol) is a synthetic and nonsteroidal estrogen, which is an estrogen receptor agonist. Estrogens can increase a normal clear discharge from the vagina and make the vulva and urethra healthy.

Ethynyl estradiol is a semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.

PHTPP is a selective ERβ antagonist.

Bavachin (Corylifolin) is a phytoestrogen that activates the estrogen receptors ERα and ERβ.

(E/Z)-Endoxifen ((E/Z)-Endoxifen) is an active metabolite of tamoxifen produced by the sequential action of cytochrome P450 (CYP) isoforms, including CYP2D6. It is a strong anti-estrogen, as it has an approximately 100-fold greater affinity for estrogen receptors than tamoxifen. As the efficient conversion of tamoxifen to endoxifen depends on CYP2D6, polymorphisms in this CYP isoform can impact the effectiveness of TMX treatment.

Melatonin (Melatonine) is a biogenic amine that is found in animals and plants. In mammals, melatonin is produced by the PINEAL GLAND. Its secretion increases in darkness and decreases during exposure to light. Melatonin is implicated in the regulation of SLEEP, mood, and REPRODUCTION. Melatonin is also an effective antioxidant.

kaempferide (4'-Methylkaempferol) inhibits the proliferation of native and estrogen receptor beta overexpressing colon cancer cells through a mechanism not mediated by ligand binding dependent estrogen receptor activation.

Estradiol benzoate (Benzhormovarine) is the synthetic benzoate ester of estradiol, a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females.

Bazedoxifene acetate (WAY-TES 424) is a novel selective estrogen receptor modulator (SERM).

Synthetic pentapeptide corresponding to the amino acids 32-36 of thymopoietin and exhibiting the full biological activity of the natural hormone. Thymopentin (TP5) is an immunomodulator which has been studied for possible use in the treatment of rheumatoid arthritis, AIDS, and other primary immunodeficiencies.