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 |
|---|---|---|---|---|
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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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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. |
|
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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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. |
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V11151 | Estradiol dipropionate | 113-38-2 | Estradiol dipropionate is an estrogen-progesterone combination that works as an estrogen and progesterone agonist. |
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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). |
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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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V20831 | Etonogestrel | 54048-10-1 | Etonogestrel (ORG3236; ORG-3236; Nexplanon; Implano; NuvaRing; Circlet) isan active metabolite of desogestrel and long-acting synthetic progestin derivative that has been used as a hormonal contraceptive drug in many devices. |
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V2297 | FLTX1 | 1481401-71-1 | FLTX1 is a fluorescent Tamoxifen derivative. |
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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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V3804 | GDC-0927 Racemate | 1443983-36-5 | GDC-0927 Racemate, the racemic mixture of GDC-0927, is used in the research of ER-related diseases. |
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V67666 | GLL398 | 2077980-80-2 | GLL398 is an orally bioactive selective estrogen receptor degrader (SERD) that competitively binds to estrogen receptors with IC50 of 1.14 nM. |
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V67714 | GNE-149 | 1953132-75-6 | GNE-149 is a potent, orally bioactive estrogen receptor alpha (ERα; IC50=0.053 nM) antagonist. |
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V67659 | GNE-274 | 2369048-69-9 | GNE-274 is a structural analog of the ER degrading agent GDC-0927 and is a non-degrading agent. |
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