Home Endocrinology & Hormones Estrogen/progestogen Receptor

Estrogen/progestogen Receptor Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
S1191 Fulvestrant (ICI-182780) Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.
Nat Genet, 2025, 57(6):1452-1462
J Clin Invest, 2025, e188839
Cell Rep Med, 2025, 6(7):102192
Verified customer review of Fulvestrant (ICI-182780)
S2606 Mifepristone (RU-486) Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.Mifepristone (RU486) can be used to induce animal models of Spontaneous Abortion.
Pharmacol Res, 2025, 215:107696
Cell Death Dis, 2025, 16(1):237
J Virol, 2025, 99(2):e0147224
Verified customer review of Mifepristone (RU-486)
S8686 PHTPP PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.
Journal of Agricultural and Food Chemistry, November 28, 2024, 28390-28399
Poultry Science, April 05, 2024, 103734
Biol Pharm Bull, 2025, 48(5):657-671
S6651 G15 G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.
Biol Pharm Bull, 2025, 48(5):657-671
iScience, 2024, 27(3):109125
Nutrients, 2023, 16(1)38
S7839 Endoxifen HCl Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Journal of Molecular Cell Biology, September 11, 2021, 433-444
ACS Omega, October 11, 2021, 27654-27667
Viruses, 2024, 16(8)1332
S0851 G-1 (LNS 8801) G-1 (LNS 8801) is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.
iScience, 2024, 109125
iScience, 2024, 27(3):109125
Poultry Science, 2024, 103734
S8746 H3B-5942 H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values of this compound are 1 nM and 0.41 nM, respectively.
Biol Pharm Bull, 2025, 48(5):657-671
Biological and Pharmaceutical Bulletin, 2025, 657-671
Nat Commun, 2024, 15(1):10170
S8687 MPP dihydrochloride Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein's interaction with ERα.
Drug Des Devel Ther, 2024, 18:4943-4960
Drug Design, Development and Therapy, 2024, 4943-4960
S8958 Camizestrant (AZD9833) Camizestrant (AZD9833) is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.
Cancer Discovery, 2024, 274-289
Viruses, 2024, 1332
Viruses, 2024, 16(8)1332
S7855 Brilanestrant (GDC-0810) Brilanestrant (GDC-0810, ARN-810) is a potent ER-α binder (ER-α, IC50 = 6.1 nM; ER-β, IC50 = 8.8 nM). This compound is a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors.
Breast Cancer Research and Treatment, 2020, 635-646
Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9
Nat Genet, 2019, 51(2):207-216
S2466 Estriol Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
Mol Cell, 2019, 75(6):1103-1116.e9
E0361 Enclomiphene Citrate

Enclomiphene citrate is the trans isomer of clomiphene citrate and acts as a non-steroidal estrogen receptor antagonist.
Biochem Pharmacol, 2024, 232:116694
E1301 Imlunestrant Imlunestrant(LY3484356) is a potent, orally bioavailable selective estrogen receptor degrader (SERD) that functions as a pure antagonist of estrogen receptor alpha (ERα). It inhibits ER-dependent gene transcription and cell proliferation, resulting in sustained suppression of estrogen-driven growth in ER-positive cells.
S8986New Giredestrant Giredestrant (GDC-9545; RG6171) is an efficient and potent selective estrogen receptor degrader and a full antagonist with an IC50 of 0.05 nM in T-47D wild-type cells. It also exhibits anti-proliferative activity.
S9609 Amcenestrant (SAR439859) Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. It is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation.
E1842 Palazestrant Palazestrant(OP-1250) is an orally bioavailable complete antagonist of estrogen receptor (ER) that blocks ER activity. It exhibits antiproliferative and antitumor activity in ER-positive (ER+) breast cancer models.