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)
- GC39630GiredestrantCAS: 1953133-47-5Purity: >99.50%
Giredestrant is an oral selective estrogen receptor (ER) degrader. Giredestrant can induce an inactive conformation of the estrogen receptor ligand binding domain and promoting proteasome-mediated degradation of the receptor protein. Giredestrant is used to treat estrogen receptor-positive (ER+) breast cancer.
- GC39747(E/Z)-GSK5182CAS: 2699724-40-6Purity: >98.50%
(E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers.
- GC40753α-ZearalanolCAS: 26538-44-3Purity: >98.00%
α-Zearalenol (α-zol) is a Mycotoxin with high affinity for the estrogen receptors (ER), α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects.
- GC44686ProchlorazCAS: 67747-09-5Purity: >98.00%
Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death.
- GC44804Raloxifene 4'-GlucuronideCAS: 182507-22-8Purity: >98.00%
Raloxifene 4'-glucuronide is a metabolite of the selective estrogen receptor modulator raloxifene.
- GC44805Raloxifene 6-GlucuronideCAS: 174264-50-7Purity: >90.00%
Raloxifene 6-glucuronide is a metabolite of the selective estrogen receptor modulator raloxifene.
- GC48124Tamoxifen-d5CAS: 157698-32-3Purity: >99.00%
An internal standard for the quantification of tamoxifen
- GC60806Enclomiphene D4 hydrochloridePurity: >98%
Enclomiphene D4 hydrochloride ((E)-Clomiphene D4 hydrochloride; trans-Clomiphene D4 hydrochloride; Enclomifene D4 hydrochloride)?is a deuterium labeled Enclomiphene.
- GC60815Estradiol dipropionateCAS: 113-38-2Purity: >98.00%
Estradiol dipropionate is a combined estrogen-progesterone, acts as an estrogen and progesterone agonist.
- GC60816Estrogen receptor modulator 1CAS: 63676-22-2Purity: >98%
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
- GC61390Zuclomiphene citrateCAS: 7619-53-6Purity: >98%
Zuclomiphene citrate is a cis isomer of Clomiphene citrate.
- GC61488(Rac)-AcolbifeneCAS: 151533-34-5Purity: >99.50%
(Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor?antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380.
- GC61514Acolbifene hydrochlorideCAS: 252555-01-4Purity: >98.00%
Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.
- GC61817GPR30 agonist-1CAS: 415919-74-3Purity: >98.50%
GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist.
- GC62307PROTAC ERRα Degrader-3CAS: 2306388-65-6Purity: >98.00%
PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
- GC62379Elacestrant (S enantiomer)CAS: 2309762-29-4Purity: >98%
Elacestrant S enantiomer (RAD1901 S enantiomer) is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
- GC62484FLTX1CAS: 1481401-71-1Purity: >99.50%
FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC38990 | Lindleyin | 59282-56-3 | >98% | |
Lindleyin, isolated from Rhei rhizoma, mediates hormonal effects through estrogen receptors. | ||||
| GC39630 | Giredestrant | 1953133-47-5 | >99.50% | |
Giredestrant is an oral selective estrogen receptor (ER) degrader. Giredestrant can induce an inactive conformation of the estrogen receptor ligand binding domain and promoting proteasome-mediated degradation of the receptor protein. Giredestrant is used to treat estrogen receptor-positive (ER+) breast cancer. | ||||
| GC39707 | Droloxifene | 82413-20-5 | >99.50% | |
A selective estrogen receptor modulator | ||||
| GC39747 | (E/Z)-GSK5182 | 2699724-40-6 | >98.50% | |
(E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. | ||||
| GC40643 | (R)-Equol | 221054-79-1 | >99.00% | |
Equol is a non-steroidal estrogen produced from the metabolism of the isoflavonoid phytoestrogen daidzein by human intestinal microflora. | ||||
| GC40753 | α-Zearalanol | 26538-44-3 | >98.00% | |
α-Zearalenol (α-zol) is a Mycotoxin with high affinity for the estrogen receptors (ER), α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects. | ||||
| GC41153 | Tibolone | 5630-53-5 | >98.00% | |
Tibolone is a synthetic steroid that possesses weak estrogenic, progestational and androgenic properties. | ||||
| GC44686 | Prochloraz | 67747-09-5 | >98.00% | |
Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. | ||||
| GC44804 | Raloxifene 4'-Glucuronide | 182507-22-8 | >98.00% | |
Raloxifene 4'-glucuronide is a metabolite of the selective estrogen receptor modulator raloxifene. | ||||
| GC44805 | Raloxifene 6-Glucuronide | 174264-50-7 | >90.00% | |
Raloxifene 6-glucuronide is a metabolite of the selective estrogen receptor modulator raloxifene. | ||||
| GC45968 | (±)-Liquiritigenin | 69097-97-8 | >95.00% | |
A flavonoid with anticancer activity | ||||
| GC48124 | Tamoxifen-d5 | 157698-32-3 | >99.00% | |
An internal standard for the quantification of tamoxifen | ||||
| GC48613 | Ospemifene-d4 | - | >99.00% | |
| GC60806 | Enclomiphene D4 hydrochloride | - | >98% | |
Enclomiphene D4 hydrochloride ((E)-Clomiphene D4 hydrochloride; trans-Clomiphene D4 hydrochloride; Enclomifene D4 hydrochloride)?is a deuterium labeled Enclomiphene. | ||||
| GC60815 | Estradiol dipropionate | 113-38-2 | >98.00% | |
Estradiol dipropionate is a combined estrogen-progesterone, acts as an estrogen and progesterone agonist. | ||||
| GC60816 | Estrogen receptor modulator 1 | 63676-22-2 | >98% | |
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors. | ||||
| GC61390 | Zuclomiphene citrate | 7619-53-6 | >98% | |
Zuclomiphene citrate is a cis isomer of Clomiphene citrate. | ||||
| GC61391 | Zuclomiphene D4 citrate | - | >98% | |
| GC61488 | (Rac)-Acolbifene | 151533-34-5 | >99.50% | |
(Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor?antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380. | ||||
| GC61514 | Acolbifene hydrochloride | 252555-01-4 | >98.00% | |
Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties. | ||||
| GC61817 | GPR30 agonist-1 | 415919-74-3 | >98.50% | |
GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist. | ||||
| GC62307 | PROTAC ERRα Degrader-3 | 2306388-65-6 | >98.00% | |
PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins. | ||||
| GC62379 | Elacestrant (S enantiomer) | 2309762-29-4 | >98% | |
Elacestrant S enantiomer (RAD1901 S enantiomer) is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. | ||||
| GC62484 | FLTX1 | 1481401-71-1 | >99.50% | |
FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus. | ||||
