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ERβ antagonists

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Androgen Receptor (2) Apoptosis (1) Calcium Channel (1) Endogenous Metabolite (3) ERK (1) Estrogen Receptor/ERR (16) Ferroptosis (1) FXR (1) G protein-coupled Bile Acid Receptor 1 (1) Glucocorticoid Receptor (1) Glutathione Reductase (GR) (1) GnRH Receptor (1) Isotope-Labeled Compounds (1) mTOR (2) NO Synthase (2) p38 MAPK (1) PI3K (1) PPAR (1) Reference Standards (1) Transmembrane Glycoprotein (1)
By Research Areas:	Cancer (12) Cardiovascular Disease (4) Endocrinology (1) Inflammation/Immunology (1) Metabolic Disease (6) Neurological Disease (2)

By Targets:

Akt (1)

Androgen Receptor (2)

Apoptosis (1)

Calcium Channel (1)

Endogenous Metabolite (3)

ERK (1)

Estrogen Receptor/ERR (16)

Ferroptosis (1)

FXR (1)

G protein-coupled Bile Acid Receptor 1 (1)

Glucocorticoid Receptor (1)

Glutathione Reductase (GR) (1)

GnRH Receptor (1)

Isotope-Labeled Compounds (1)

mTOR (2)

NO Synthase (2)

p38 MAPK (1)

PI3K (1)

PPAR (1)

Reference Standards (1)

Transmembrane Glycoprotein (1)

By Research Areas:

Cancer (12)

Cardiovascular Disease (4)

Endocrinology (1)

Inflammation/Immunology (1)

Metabolic Disease (6)

Neurological Disease (2)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-103456

PHTPP Maximum Cited Publications 30 Publications Verification	Estrogen Receptor/ERR	Cancer
PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα .

HY-B0412

Estriol 5 Publications Verification Oestriol	Estrogen Receptor/ERR Endogenous Metabolite	Cancer
Estriol (Oestriol), an orally active estrogen, is a ERα and *ERβ* agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .

HY-15731

Estetrol	Estrogen Receptor/ERR Endogenous Metabolite NO Synthase	Cardiovascular Disease Cancer
Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .

HY-114263

NXT629 4 Publications Verification	PPAR	Cancer
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC₅₀ of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC₅₀s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively . NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models .

HY-16023A

Acolbifene 2 Publications Verification EM-652; SCH 57068	Estrogen Receptor/ERR	Cancer
Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC₅₀ = 2 nM) and ERβ (IC₅₀ = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties .

HY-N0910

Notoginsenoside Ft1 1 Publications Verification	PI3K mTOR Akt Apoptosis p38 MAPK ERK Transmembrane Glycoprotein Glutathione Reductase (GR) Estrogen Receptor/ERR Calcium Channel Ferroptosis G protein-coupled Bile Acid Receptor 1 FXR	Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Notoginsenoside Ft1 is an orally active bioactive saponin. Notoginsenoside Ft1 inhibits the PI3K/AKT/mTOR signaling pathway, activates the p38 MAPK and ERK1/2 signaling pathways, and increases the proportion of CD8 ⁺ T cells, thereby inducing apoptosis and lysosomal cell death in various cancer cells, and promoting angiogenesis. Notoginsenoside Ft1 causes vasodilation by activating glucocorticoid receptors (GR) and estrogen receptor beta (ERβ) in endothelial cells. Notoginsenoside Ft1 increases intracellular Ca ²⁺ accumulation, reduces cAMP levels by activating a signaling network mediated through P2Y₁₂ receptors, and promotes platelet aggregation, thereby exerting a procoagulant effect. Notoginsenoside Ft1 inhibits ferroptosis (ferroptosis) in renal tubular epithelial cells by activating the TGR5 receptor, thereby demonstrating a renal protective effect. Notoginsenoside Ft1 acts as a TGR5 agonist and an FXR antagonist to combat obesity and insulin resistance .

HY-103457

Y134	Estrogen Receptor/ERR	Cancer
Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and *ERβ. Y134 shows 121.1-fold selectivity for ERα (K_i=0.09 nM) over ERβ* (K_i=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .

HY-P4190

Fsh receptor-binding inhibitor fragment(bi-10)	GnRH Receptor	Endocrinology
FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries .

HY-150693

*Estrogen receptor β antagonist* 2**	Estrogen Receptor/ERR	Cancer
Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC₅₀s of 109.10, 0.63 µM for Erα and Erβ, respectively .

HY-W114419

Bisphenol C	Estrogen Receptor/ERR mTOR	Cardiovascular Disease Metabolic Disease
Bisphenol C is an estrogen receptor-α (ERα) agonist and an *ERβ* antagonist, with IC₅₀ values of 2.65 nM for ERα and 1.94 nM for ERβ. Bisphenol C is a material of manufacturing polyester polymers like polycarbonate, is widely used in daily items like water bottles, food packaging, textile and so on .

HY-125627

CP-394531	Glucocorticoid Receptor Androgen Receptor	Neurological Disease Metabolic Disease
CP-394531 is an efficient and highly selective non-steroidal glucocorticoid receptor (GR) antagonist, with a K_i value of 0.1 nM. CP-394531 has a weak binding to androgen receptor (AR) (K_i = 130 nM), and has almost no effect on progesterone receptor (PR) and estrogen receptors (ERα, ERβ). CP-394531 completely blocks the half-maximal agonistic effect induced by Dexamethasone (HY-14648G), with a K_if of 4.1 nM. CP-394531 can be used to study various diseases such as diabetes, obesity, depression, neurodegenerative diseases, glaucoma and Cushing's disease .

HY-169941

*ERα/ERβ* antagonist-1**	Estrogen Receptor/ERR	Metabolic Disease Cancer
ERα/ERβ antagonist-1 (Compound 10) is partial antagonists of ERα and *ERβ. ERα/ERβ* antagonist-1 reduces ERα and *ERβ* activity in a dose-dependent manner in HepG2 liver cells .

HY-173474

*ERβ agonist-1*	Estrogen Receptor/ERR Androgen Receptor	Cancer
ERβ agonist-1 (Compound 8) is a dual-active selective *ERβ* agonist (EC₅₀: 46.8 nM) and AR antagonist (IC₅₀: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer .

HY-103451

(R,R)-THC	Estrogen Receptor/ERR	Metabolic Disease
(R,R)-THC is an ERα agonist and an ERβ antagonist, with K_is of 9.0 nM and 3.6 nM for ERα and ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ than ERα with the values of 25 and 3.6 .

HY-103451A

rel-(R,R)-THC	Estrogen Receptor/ERR	Metabolic Disease
rel-(R,R)-THC is the relative configuration of (R,R)-THC (HY-103451). (R,R)-THC is an ERα agonist and an *ERβ* antagonist, with K_is of 9.0 nM and 3.6 nM for ERα and *ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ* than ERα with the values of 25 and 3.6 .

HY-103456R

PHTPP (Standard)	Reference Standards Estrogen Receptor/ERR	Cancer
PHTPP (Standard) is the analytical standard of PHTPP. This product is intended for research and analytical applications. PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα .

HY-114631

EM-800	Estrogen Receptor/ERR	Cancer
EM-800, an orally active anti-estrogen, serves as an antagonist to the transcriptional functions of estrogen receptors α (ERα) and β (ERβ). EM-800 possesses anticancer activity, capable of inhibiting the growth of breast cancer induced by 7,12-Dimethylbenz[a]anthracene (DMBA) (HY-W011845). Furthermore, in ovariectomized animals, EM-800 effectively slows down bone loss. Additionally, EM-800 shows potential in the research of breast and endometrial cancers, while exerting beneficial effects on bone and lipid metabolism .

HY-15731S1

Estetrol-d4 (Major)	Isotope-Labeled Compounds NO Synthase Endogenous Metabolite Estrogen Receptor/ERR	Cardiovascular Disease
Estetrol-d₄ (Major) is the deuterium labeled Estetrol (HY-15731). Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .

HY-164726

Estrogen receptor modulator 11	Estrogen Receptor/ERR	Others
Estrogen receptor modulator 11 (Compound 27) is a tetrahydroisoquinoline derivative. Estrogen receptor modulator 11 has a certain affinity for estrogen receptors (ER), with IC₅₀ values of 285 nM and 421 nM for ERα and *ERβ, respectively. Estrogen receptor modulator 11 lacks antagonist* activity in the MCF-7 cellular assay .

Cat. No.	Product Name	Target	Research Area

HY-P4190

Fsh receptor-binding inhibitor fragment(bi-10)	GnRH Receptor	Endocrinology
FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0412

Estriol 5 Publications Verification Oestriol	Monophenols Immune System Disorder Classification of Application Fields Disease markers Phenols Endocrine diseases Endogenous metabolite Disease Research Fields Steroids Cancer Source Classification	Estrogen Receptor/ERR Endogenous Metabolite
Estriol (Oestriol), an orally active estrogen, is a ERα and *ERβ* agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .

HY-15731

Estetrol	Cardiovascular Disease Monophenols Classification of Application Fields Phenols Endogenous metabolite Disease Research Fields Steroids Source Classification	Estrogen Receptor/ERR Endogenous Metabolite NO Synthase
Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .

HY-N0910

Notoginsenoside Ft1 1 Publications Verification	Triterpenes Structural Classification Panax notoginseng (Burkill) F. H. Chen ex C. H. Chow Classification of Application Fields Terpenoids Other Diseases Plants Disease Research Fields Araliaceae Source Classification	PI3K mTOR Akt Apoptosis p38 MAPK ERK Transmembrane Glycoprotein Glutathione Reductase (GR) Estrogen Receptor/ERR Calcium Channel Ferroptosis G protein-coupled Bile Acid Receptor 1 FXR
Notoginsenoside Ft1 is an orally active bioactive saponin. Notoginsenoside Ft1 inhibits the PI3K/AKT/mTOR signaling pathway, activates the p38 MAPK and ERK1/2 signaling pathways, and increases the proportion of CD8 ⁺ T cells, thereby inducing apoptosis and lysosomal cell death in various cancer cells, and promoting angiogenesis. Notoginsenoside Ft1 causes vasodilation by activating glucocorticoid receptors (GR) and estrogen receptor beta (ERβ) in endothelial cells. Notoginsenoside Ft1 increases intracellular Ca ²⁺ accumulation, reduces cAMP levels by activating a signaling network mediated through P2Y₁₂ receptors, and promotes platelet aggregation, thereby exerting a procoagulant effect. Notoginsenoside Ft1 inhibits ferroptosis (ferroptosis) in renal tubular epithelial cells by activating the TGR5 receptor, thereby demonstrating a renal protective effect. Notoginsenoside Ft1 acts as a TGR5 agonist and an FXR antagonist to combat obesity and insulin resistance .

Cat. No.	Product Name	Chemical Structure

HY-15731S1

Estetrol-d4 (Major)
Estetrol-d₄ (Major) is the deuterium labeled Estetrol (HY-15731). Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .

Estetrol-d4 (Major)

Estetrol-d₄ (Major) is the deuterium labeled Estetrol (HY-15731). Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .

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ERβ antagonists

Inhibitors & Agonists

Peptides

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Isotope-Labeled Compounds

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