Estrogen Receptor/ERR
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Estrogen receptors are a group of proteins found inside cells. They are receptors that are activated by the hormone estrogen (17β-estradiol). Two classes of estrogen receptor exist: ER, which is a member of the nuclear hormone family of intracellular receptors, and GPER (GPR30), which is a member of the rhodopsin-like family of G protein-coupled receptors. The ER's helix 12 domain plays a crucial role in determining interactions with coactivators and corepressors and, therefore, the respective agonist or antagonist effect of the ligand. Different ligands may differ in their affinity for alpha and beta isoforms of the estrogen receptor: estradiol binds equally well to both receptors, estrone, and raloxifene bind preferentially to the alpha receptor, estriol, and genistein to the beta receptor. Estrogen and its receptors are essential for sexual development and reproductive function, but also play a role in other tissues such as bone. Estrogen receptors are also involved in pathological processes including breast cancer, endometrial cancer, and osteoporosis. Alternative promoter usage and alternative splicing result in dozens of transcript variants, but the full-length nature of many of these variants has not been determined.
Products Related to Estrogen Receptor/ERR(175)
- GC10002CoumestrolCAS: 479-13-0Purity: >98.00%
Coumestrol is a natural, orally active coumestan phytoestrogen. Coumestrol competitively binds estrogen receptor ERα (IC 50 =11nM) and ERβ (IC 50 =2nM) to regulate estrogen-responsive genes.
- GC10389ERB 041CAS: 524684-52-4Purity: >98.00%
ERB 041 (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. ERB 041 displays >200-fold selectivity for ERβ over ERα. ERB 041 is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. ERB 041 induces ovarian cancer apoptosis.
- GC11425Lasofoxifene (tartrate)CAS: 190791-29-8Purity: >99.50%
third-generation, non-steroidal selective estrogen receptor modulator (SERM)
- GC11796Estradiol valerateCAS: 979-32-8Purity: >99.00%
Estradiol valerate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy drugs.
- GC11822Erteberel (LY500307)CAS: 533884-09-2Purity: >98.00%
Erteberel (LY500307) (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively.
- GC11863PHTPPCAS: 805239-56-9Purity: >98.00%
PHTPP is a selective ERβ full antagonist with 36-fold selectivity for ERβ over ERα. PHTPP can selectively antagonize the ligand binding and transcriptional functions of ERβ, blocking its inhibitory effect on tumor cells, thereby promoting cell proliferation. PHTPP was used to verify ERβ function.
- GC11996OspemifeneCAS: 128607-22-7Purity: >99.50%
non-hormonal selective estrogen receptor modulator (SERM)
- GC12148Ethinyl EstradiolCAS: 57-63-6Purity: >99.50%
Ethinyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
- GC12644QuinestrolCAS: 152-43-2Purity: >98.00%
synthetic estrogen that is effective in hormone replacement therapy
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC10002 | Coumestrol | 479-13-0 | >98.00% | |
Coumestrol is a natural, orally active coumestan phytoestrogen. Coumestrol competitively binds estrogen receptor ERα (IC 50 =11nM) and ERβ (IC 50 =2nM) to regulate estrogen-responsive genes. | ||||
| GC10139 | Estradiol Cypionate | 313-06-4 | >98.00% | |
Estrogen receptor inhibitor | ||||
| GC10389 | ERB 041 | 524684-52-4 | >98.00% | |
ERB 041 (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. ERB 041 displays >200-fold selectivity for ERβ over ERα. ERB 041 is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. ERB 041 induces ovarian cancer apoptosis. | ||||
| GC10394 | DY131 | 95167-41-2 | >98.00% | |
An ERRβ/γ agonist | ||||
| GC10558 | GSK 4716 | 101574-65-6 | >98.00% | |
estrogen-related receptors ERRβ and ERRγ agonist | ||||
| GC10684 | Zearalanone | 5975-78-0 | >98.00% | |
estrogen receptor agonist | ||||
| GC10789 | XCT790 | 725247-18-7 | >98.00% | |
XCT790 is a potent and selective inverse agonist for ERRα with an IC 50 value of 0.37μM. | ||||
| GC10852 | Bazedoxifene acetate | 198481-33-3 | >99.50% | |
A selective estrogen receptor modulator | ||||
| GC11215 | Diethylstilbestrol | 56-53-1 | >99.00% | |
synthetic nonsteroidal estrogen | ||||
| GC11282 | β-Estradiol | 50-28-2 | >99.50% | |
Sex hormone | ||||
| GC11425 | Lasofoxifene (tartrate) | 190791-29-8 | >99.50% | |
third-generation, non-steroidal selective estrogen receptor modulator (SERM) | ||||
| GC11544 | Toremifene | 89778-26-7 | >98% | |
| GC11669 | Tamoxifen Citrate | 54965-24-1 | >99.50% | |
Antiestrogen drug | ||||
| GC11734 | α-Zearalenol | 36455-72-8 | >98.00% | |
estrogen receptor agonist | ||||
| GC11796 | Estradiol valerate | 979-32-8 | >99.00% | |
Estradiol valerate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy drugs. | ||||
| GC11822 | Erteberel (LY500307) | 533884-09-2 | >98.00% | |
Erteberel (LY500307) (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. | ||||
| GC11863 | PHTPP | 805239-56-9 | >98.00% | |
PHTPP is a selective ERβ full antagonist with 36-fold selectivity for ERβ over ERα. PHTPP can selectively antagonize the ligand binding and transcriptional functions of ERβ, blocking its inhibitory effect on tumor cells, thereby promoting cell proliferation. PHTPP was used to verify ERβ function. | ||||
| GC11996 | Ospemifene | 128607-22-7 | >99.50% | |
non-hormonal selective estrogen receptor modulator (SERM) | ||||
| GC12140 | Endoxifen | 112093-28-4 | >98% | |
Endoxifen Z-isomer is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). | ||||
| GC12148 | Ethinyl Estradiol | 57-63-6 | >99.50% | |
Ethinyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. | ||||
| GC12182 | Estriol | 50-27-1 | >99.00% | |
Estriol is an agonist of estrogen receptors (ERα and ERβ) and G protein-coupled receptor 30 (GPR30) antagonist. | ||||
| GC12644 | Quinestrol | 152-43-2 | >98.00% | |
synthetic estrogen that is effective in hormone replacement therapy | ||||
| GC12766 | G-1 | 881639-98-1 | >99.50% | |
G-1 is a selective and potent agonist of GPR30 with EC50 value about 2 nM. | ||||
| GC13309 | WAY 200070 | 440122-66-7 | >99.00% | |
ERβ receptor agonist | ||||
