Estrogen receptors are a group of proteins found inside cells.They are receptors that the estrogen (17-estradiol) hormone activates. There are two classes of estrogen receptors: GPER (GPR30), a member of the rhodopsin-like family of G protein-coupled receptors, and ER, a member of the nuclear hormone family of intracellular receptors. The interactions between coactivators and corepressors, and consequently, the agonist or antagonist effect of the ligand, are heavily influenced by the ER's helix 12 domain.Different ligands may have different affinities for the estrogen receptor's alpha and beta isoforms. Estradiol binds to both receptors equally well, however raloxifene, estrone, and genistein bind preferentially to the alpha receptor. In addition to being necessary for sexual maturation and reproductive function, estrogen and its receptors also affect other tissues, like bone. In pathological conditions like osteoporosis, endometrial cancer, and breast cancer, estrogen receptors play a role. Numerous transcript variations are produced by alternative promoter use and alternative splicing, however it is unknown how many of these variants are full-length.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V19820 | Dienestrol | 84-17-3 | Dienestrol is a synthetic, non-steroidal estrogen acting as an estrogen receptor agonist for the treatment of menopausal and postmenopausal symptoms. |
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V5719 | Endoxifen Z-isomer | 112093-28-4 | Endoxifen Z-isomer is an active metabolite of Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). |
|
V20253 | Droloxifene (3-Hydroxytamoxifen) | 82413-20-5 | Droloxifene (3-Hydroxytamoxifen) is a tamoxifen analogue and orally bioactive SERM (selective estrogen receptor modulator) that acts as an ER agonist in bone and as an ER antagonist in breast tissue. |
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V1994 | Kaempferol (Kempferol; Robigenin) | 520-18-3 | Kaempferol (Kempferol; Robigenin), a naturally occuring flavonoid analog, is a potent ERRα (estrogen receptor α) and ERRγ inverse agonist. |
|
V2995 | Brilanestrant | 1365888-06-7 | Brilanestrant (formerly known as GDC-0810, ARN-810 and/or RG6046) isa novel, potent and orally bioavailable Selective Estrogen Receptor Degrader (SERD) that demonstrates robust activity inmodels of tamoxifen-sensitive and tamoxifen-resistant breast cancer, and is currently in clinical trials in women with locally advanced or metastatic estrogen receptor-positive breast cancer. |
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V33910 | Endoxifen | 110025-28-0 | Endoxifen, an active metabolite of Tamoxifen, is a potent and selective estrogen receptor antagonist and has been found to be effective in patients that have failed previous hormonal therapies. |
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V19199 | Enclomiphene citrate | 7599-79-3 | Enclomiphene citrate, formerly known as ICI-46476, RMI-16289 and trans-Clomiphene, is an orally bioavailable non-steroidal estrogen receptor antagonist in development for secondary hypogonadism in overweight men wishing to restore normal testicular function. |
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V18266 | Chrysin | 480-40-0 | Chrysin is an estrogen blocker. |
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V20734 | Estradiol Benzoate | 50-50-0 | Estradiol Benzoate, the 3-benzoylated form of Estradiol, is a prodrug of estradiol which acts as a steroid sex hormone while exhibiting mild anabolic and metabolic properties and increasing blood coagulability. |
|
V2047 | Avobenzone (BF2AVB) | 70356-09-1 | AZD9496 is a novel, potent, orally bioavailable, and selective estrogen receptor (ERα) downregulator and antagonist with an IC50 of 0.28 nM and a Ki of 0.7 nM. AZD9496 showed pmol/L equipotent binding to both ERα and ERβ isoforms. |
|
V4677 | Acolbifene (EM 652; SCH 57068) | 182167-02-8 | Acolbifene (also known as EM-652 and SCH-57068) is a novel, potent and selective estrogen receptor modulator/antatonist (SERM) with a IC50 value of 22±3 nM. |
|
V20738 | Estropipate (piperazine estrone sulfate) | 7280-37-7 | Estropipate (formerly piperazine estrone sulfate), a form of estrogen and an estrogen receptor agonist, is a female sex hormone produced by the ovaries. Estrogen is necessary for many processes in the body. |
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V28146 | Equol (racemic) | 94105-90-5 | Equol (racemic), the racemic mixture of equol,is a drug is potentially for the treatment of acute thyroid disease and inhibits proliferation of human gastric carcinoma cells. |
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V30482 | Equilin (7-Dehydroestrone) | 474-86-2 | Equilin (7-Dehydroestrone) is an important member of a large family of estrogenic substances that is chemically related to estradiol. |
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