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- Clomifene inhibits estrogen receptors in hypothalamus, inhibiting negative feedback of estrogen on gonadotropin release, leading to up-regulation of the hypothalamic-Cpituitary-Cadrenal axis.
- Raloxifene is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women.
- Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
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Aromatase inhibitor
Fulvestrant is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor.- Samy A. F. Morad, .et al. , Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Kaneyasu Nishimura, .et al. , Stem Cell Reports, 2016, Apr 12; 6(4): 511-524 PMID: 26997644
- Alejandro S. Cazzulino, .et al. , Hippocampus, 2016, Jun; 26(6): 752-762 PMID: 26662713
- Rie Mukai, .et al. , Am J Physiol Regul Integr Comp Physiol, 2016, Dec 1;311(6):R1022-R1031 PMID: 27629889
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
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GPR119 agonist
GSK-1292263 is a novel GPR119 agonist.- Inoue A, .et al. , Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
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ERRα and ERRγ inverse agonist
Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.- A O Hamouda, .et al. , Eur Rev Med Pharmacol Sci, 2022, Dec;26(23):8644-8659 PMID: 36524484
- Mifepristone, an antioxidant and glucocorticoid receptor antagonist, demonstrates the ability to suppress activation of NFκB, a nuclear transcription factor that affects the expression of various adhesion molecules and several inflammatory genes.
- Shuang Liang, .et al. , Cardiovasc Ther, 2022, Apr 7;2022:7145699 PMID: 35474714
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Estrogen receptor antagonist
Tamoxifen Citrateis a selective and potent inhibitor of mammalian sterol isomerase.- Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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estrogen-receptor modulator
Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 ?M and 2.6 ?M, respectively. -
estrogen agonist
Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist. - Liquiritigenin is a plant-derived highly selective estrogen receptor ?? agonist
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Estrogen receptor antagonist
(E/Z)-4-hydroxy Tamoxifen 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.- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Estrogen receptor antagonist
Endoxifen is a secondary metabolite of tamoxifen. It is a primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer.- Marina Arino Martin, .et al. , Environ Res, 2021, Apr 3;197:111121 PMID: 33823193
- Martin MA, .et al. , Water Res, 2019, Dec 29;171:115451 PMID: 31901682
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ERα agonist
Propyl pyrazole triol (PPT) is an estrogen receptor alpha (ERα) agonist. - Zearalenone is a phytoestrogenic mycotoxin usually produced by Fusarium species, is shown to be a cytotoxic compound, but alos binds to the estrogen receptor (ER) (IC50 values are 166 and 240 nM for ERβ and ERα respectively) and was found to stimulate the transcriptional activity of both subtypes at concentrations between 1 - 10 nM.
- Muthulakshmi S, .et al. , J Appl Toxicol, 2018, Nov;38(11):1388-1397 PMID: 29923290
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estrogen receptor modulator
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM). -
Estrogen modulator
Bazedoxifene is a third generation selective modulator of estrogen receptor. -
Estrogen receptor modulator
Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. -
ERRβ & ERRγ Agonist
GSK4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
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Estrogen receptor agonist
(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.- Gao X, .et al. , Toxins (Basel), 2020, Jan 26;12(2) PMID: 31991913
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Estrogen receptor ligand
α-Estradiol is an endogenous estrogen receptor ligand (Ki values are 0.2 and 1.2 nM for ERα and ERβ receptors respectively). - Estropipate is a form of estrogen, an estrogen receptor agonist. It has several uses such as: Alleviate symptoms of menopause as hormone replacement therapy, treatment some types of infertility, treatment of some conditions leading to underdevelopment of female sexual characteristics, and treatment of prostate cancer and prevention of osteoporosis.
- Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
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selective Estrogen receptor modulator
Lasofoxifene tartrate is a third-generation selective estrogen receptor modulator. -
ERRγ agonist
GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
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Smurf1 inhibitor
Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation. -
ERRβ agonist
WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM. - (-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
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estrogen receptor modulator
4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM). -
estrogen receptor (ERα) antagonist
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD). -
oestrogen receptor antagonist
Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property. -
ERRα agonist
Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist. -
Estrogen receptor degrader
SAR439859 is an orally available, nonsteroidal selective estrogen receptor degrader/downregulator (SERD).
