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)
- GC30650ERB-196 (WAY-202196)CAS: 550997-55-2Purity: >98%
ERB-196 (WAY-202196) is a nonsteroidal selective estrogen receptor-β (ERβ) agonist.
- GC31008DienestrolCAS: 84-17-3Purity: >98.00%
Dienestrol is a synthetic, non-steroidal estrogen, is an estrogen receptor agonist, for the treatment of menopausal and postmenopausal symptoms.
- GC31565NNC45-0781CAS: 207277-66-5Purity: >98%
NNC45-0781 is a tissue-selective estrogen partial-agonist.
- GC31589MK-6913 (Tetrahydrofluoroene 52)CAS: 1398510-92-3Purity: >98%
MK-6913 (Tetrahydrofluoroene 52) (Tetrahydrofluoroene 52) is a potent and selective estrogen receptor β agonist.
- GC31746Gestrinone (R 2323)CAS: 16320-04-0Purity: >99.00%
An androgen and progesterone receptor ligand used to treat endometriosis
- GC32445Nitromifene (CI628)CAS: 10448-84-7Purity: >98%
Nitromifene (CI628) is an antagonist of estrogen receptor (ER).
- GC32696Elacestrant dihydrochloride (RAD1901 dihydrochloride)CAS: 1349723-93-8Purity: >99.50%
Elacestrant dihydrochloride (RAD1901 dihydrochloride) is a novel, orally bioavailable selective estrogen receptor (ER) degrader with IC 50 of 48nM and 870nM for ERα and ERβ, respectively.
- GC32782Brilanestrant (ARN-810)CAS: 1365888-06-7Purity: >99.50%
Brilanestrant (ARN-810) (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
- GC32920GDC-0927 (SRN-927)CAS: 1642297-01-5Purity: >99.50%
GDC-0927 (SRN-927) (SRN-927) is a potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist.
- GC33025Elacestrant (RAD1901)CAS: 722533-56-4Purity: >98%
Elacestrant (RAD1901) (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
- GC33193GDC-0927 Racemate (SRN-927 Racemate)CAS: 1443983-36-5Purity: >98%
GDC-0927 Racemate (SRN-927 Racemate) (SRN-927 Racemate) is a degrader of estrogen receptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases.
- GC33349E3 ligase Ligand 5CAS: 1264754-13-3Purity: >98.00%
E3 ligase Ligand 5 is an estrogen-related receptor α (ERRα) antagonist with IC50s of 0.04 and 2.8 μM for ERRα and ERRγ, respectively.
- GC33378H3B-6545 HydrochlorideCAS: 2052132-51-9Purity: >99.00%
H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.
- GC33381Arzoxifene hydrochloride (LY 353381 HCl)CAS: 182133-27-3Purity: >98%
Arzoxifene (LY353381) hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
- GC33402Idoxifene (CB7432)CAS: 116057-75-1Purity: >98%
Idoxifene (CB7432) (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM).
- GC34006Equilin (7-Dehydroestrone)CAS: 474-86-2Purity: >99.00%
Equilin (7-Dehydroestrone) (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone).
- GC34153Pipendoxifene hydrochlorideCAS: 245124-69-0Purity: >99.00%
Pipendoxifene hydrochloride is a selective estrogen receptor modulator (SERM) that can be used for the research of breast cancer.
- GC34341PROTAC ERα Degrader-1CAS: 2417369-94-7Purity: >98%
PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC30650 | ERB-196 (WAY-202196) | 550997-55-2 | >98% | |
ERB-196 (WAY-202196) is a nonsteroidal selective estrogen receptor-β (ERβ) agonist. | ||||
| GC31008 | Dienestrol | 84-17-3 | >98.00% | |
Dienestrol is a synthetic, non-steroidal estrogen, is an estrogen receptor agonist, for the treatment of menopausal and postmenopausal symptoms. | ||||
| GC31565 | NNC45-0781 | 207277-66-5 | >98% | |
NNC45-0781 is a tissue-selective estrogen partial-agonist. | ||||
| GC31589 | MK-6913 (Tetrahydrofluoroene 52) | 1398510-92-3 | >98% | |
MK-6913 (Tetrahydrofluoroene 52) (Tetrahydrofluoroene 52) is a potent and selective estrogen receptor β agonist. | ||||
| GC31746 | Gestrinone (R 2323) | 16320-04-0 | >99.00% | |
An androgen and progesterone receptor ligand used to treat endometriosis | ||||
| GC32406 | H3B-6545 | 2052130-80-8 | >99.50% | |
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer. | ||||
| GC32445 | Nitromifene (CI628) | 10448-84-7 | >98% | |
Nitromifene (CI628) is an antagonist of estrogen receptor (ER). | ||||
| GC32696 | Elacestrant dihydrochloride (RAD1901 dihydrochloride) | 1349723-93-8 | >99.50% | |
Elacestrant dihydrochloride (RAD1901 dihydrochloride) is a novel, orally bioavailable selective estrogen receptor (ER) degrader with IC 50 of 48nM and 870nM for ERα and ERβ, respectively. | ||||
| GC32782 | Brilanestrant (ARN-810) | 1365888-06-7 | >99.50% | |
Brilanestrant (ARN-810) (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM. | ||||
| GC32920 | GDC-0927 (SRN-927) | 1642297-01-5 | >99.50% | |
GDC-0927 (SRN-927) (SRN-927) is a potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist. | ||||
| GC33011 | BHPI | 56632-39-4 | >98.00% | |
An ERα antagonist | ||||
| GC33025 | Elacestrant (RAD1901) | 722533-56-4 | >98% | |
Elacestrant (RAD1901) (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. | ||||
| GC33193 | GDC-0927 Racemate (SRN-927 Racemate) | 1443983-36-5 | >98% | |
GDC-0927 Racemate (SRN-927 Racemate) (SRN-927 Racemate) is a degrader of estrogen receptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases. | ||||
| GC33262 | H3B-5942 | 2052128-15-9 | >98.00% | |
A selective estrogen receptor covalent antagonist | ||||
| GC33349 | E3 ligase Ligand 5 | 1264754-13-3 | >98.00% | |
E3 ligase Ligand 5 is an estrogen-related receptor α (ERRα) antagonist with IC50s of 0.04 and 2.8 μM for ERRα and ERRγ, respectively. | ||||
| GC33378 | H3B-6545 Hydrochloride | 2052132-51-9 | >99.00% | |
H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer. | ||||
| GC33381 | Arzoxifene hydrochloride (LY 353381 HCl) | 182133-27-3 | >98% | |
Arzoxifene (LY353381) hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol. | ||||
| GC33402 | Idoxifene (CB7432) | 116057-75-1 | >98% | |
Idoxifene (CB7432) (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM). | ||||
| GC34006 | Equilin (7-Dehydroestrone) | 474-86-2 | >99.00% | |
Equilin (7-Dehydroestrone) (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone). | ||||
| GC34151 | PAC | 2158322-33-7 | >98.00% | |
PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab). | ||||
| GC34153 | Pipendoxifene hydrochloride | 245124-69-0 | >99.00% | |
Pipendoxifene hydrochloride is a selective estrogen receptor modulator (SERM) that can be used for the research of breast cancer. | ||||
| GC34293 | Elacestrant S enantiomer (RAD1901 S enantiomer) | - | >98% | |
| GC34294 | Elacestrant S enantiomer dihydrochloride (RAD1901 S enantiomer dihydrochloride) | - | >98% | |
| GC34341 | PROTAC ERα Degrader-1 | 2417369-94-7 | >98% | |
PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader. | ||||
