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 |
|---|---|---|---|---|
|
V67712 | ER degrader 6 | 2922929-62-0 | ER degrader 6 (compound 35s) is a potent estrogen receptor (ER) alpha degrader. |
|
V84704 | ER degrader 8 | ||
|
V67721 | ERRα antagonist-1 | 1072145-33-5 | ERRα antagonist-1 (Compound A) is a selective, high-affinity estrogen-related receptor α (ERRα) antagonist. |
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V67719 | ERRγ inverse agonist 1 | 2316832-86-5 | ERRγ Inverse Agonist 1 (Compound 12) is a specific, orally bioactive estrogen-related receptor gamma (ERRγ) inverse agonist/activator with IC50 of 40 nM. |
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V67725 | ERRγ inverse agonist 2 | 324022-01-7 | ERRγ inverse agonist 2 (compound 19) is a potent and specific ERRγ inverse agonist/activator with a Kd of 6.5 μM. |
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V94988 | ERα degrader 10 | ERα degrader 10 is a potent, selective and orally available estrogen receptor α (ERα) degrader. | |
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V94379 | ERα degrader 11 | 3052336-87-2 | ERα degrader 11 (Compound B16) is a selective ERα degrader that can be used as an estrogen receptor probe to study the ER status in ER-positive breast cancer cells. |
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V67716 | ERα degrader 5 | 2941268-96-6 | ERα degrader 5 (Compound 40) is a selective, orally bioactive estrogen receptor (ER) degrader with EC50 of 1.1 nM for ERα. |
|
V101797 | ERα degrader 8 | 2971837-95-1 | ERα degrader 8 (compound 18j) is a selective estrogen receptor degrader. |
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V67717 | ERα degrader-2 | 2235396-63-9 | ERα degrader-2 is a selective estrogen receptor degrader (SERD) with strong binding affinity to ERα (IC50=17.1 nM) and good degradation effect (EC50=0.3 nM). |
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V67702 | Estradiol enanthate | 4956-37-0 | Estradiol enanthate is a short-acting estrogen. |
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V67674 | Estrogen receptor antagonist 7 | 2889371-04-2 | Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptor (ER) antagonist. |
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V67709 | Estrogen receptor antagonist 8 | 2889370-92-5 | Estrogen receptor blocker (antagonist) 8 is a potent estrogen receptor ER antagonist (inhibitor) with antiuterine properties in vivo (EC50=4.160 μM) |
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V67718 | Estrogen receptor modulator 6 | 787621-78-7 | Estrogen receptor modulator 6 (compound 3a) is a selective estrogen receptor ERβ agonist (Ki=0.44 nM). |
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V67677 | Estrogen receptor modulator 7 | 2639168-13-9 | Estrogen receptor modulator 7 is a potent estrogen receptor modulator. |
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V67680 | Estrogen receptor modulator 8 | 2170766-56-8 | Estrogen receptor modulator 8 (compound 4) is an orally bioactive estrogen receptor/ERR alpha inhibitor (IC50=0.437 nM, MCF-7 cells). |
|
V2297 | FLTX1 | 1481401-71-1 | FLTX1 is a fluorescent Tamoxifen derivative. |
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V103354 | FSH receptor antagonist 1 | 487064-35-7 | FSH receptor antagonist 1 (compound 10) is a potent antagonist of the G(s) protein-coupled human follicle-stimulating hormone (FSH) receptor. |
|
V67653 | FSHR agonist 1 | 1256776-89-2 | FSHR agonist 1 is a high-affinity and allosteric follicle-stimulating hormone (FSH) receptor (FSHR) agonist/activator with pEC50 of 7.72. |
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V3803 | GDC-0927 | 1642297-01-5 | GDC-0927 (formerly known as SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective ER (estrogen receptor) antagonist/ER degrader (SERD) that induces tumor regression in ER+ BC patient-derived xenograft models. |
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