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Isoforms Recommended:	ERβ

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ERβ

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (3) EGFR (1) Endogenous Metabolite (1) Estrogen Receptor/ERR (12) GnRH Receptor (1) PPAR (1)
By Research Areas:	Cancer (13) Cardiovascular Disease (1) Endocrinology (3) Infection (1) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (1)

16

Inhibitors & Agonists

1

Peptides

3

Natural
Products

1

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

OP-1074	Estrogen Receptor/ERR	Cancer
OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC₅₀ of 1.6 and 3.2 nM, respectively .

(R)-OP-1074	Others	Cancer
(R)-OP-1074 is the isomer of OP-1074 (HY-125263), and can be used as an experimental control. OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC₅₀ of 1.6 and 3.2?nM, respectively .

Ferutinin	Estrogen Receptor/ERR Apoptosis	Infection Inflammation/Immunology Endocrinology Cancer
Ferutinin, a natural terpenoid compound, is an estrogen receptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC₅₀s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca ²⁺-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities .

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-146742

PPARγ agonist 2

PPAR Metabolic Disease

PPARγ agonist 2 is a potent PPARγ partial agonist and can be used for metabolic disease research .

Acolbifene 1 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 .

Ospemifene D4 FC-1271a d₄	Estrogen Receptor/ERR	Cancer
Ospemifene-d₄ is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects[1][2].

Acolbifene hydrochloride 1 Publications Verification EM-652 hydrochloride; SCH 57068 hydrochloride	Estrogen Receptor/ERR	Cancer
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 .

AC-186	Estrogen Receptor/ERR	Neurological Disease
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC₅₀s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease .

Estriol 3 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 .

(±)-8-Prenylnaringenin	Estrogen Receptor/ERR Apoptosis	Metabolic Disease Endocrinology Cancer
(±)-8-Prenylnaringenin, a natural prenylated flavonoid, is a potent phytoestrogen. (±)-8-Prenylnaringenin is an orally active selective estrogen receptor modulator (SERM) (Estrogen Receptor/ERR) that inhibits ERα and ERβ with IC₅₀s of 57 nM and 68 nM, respectively. (±)-8-Prenylnaringenin has anticancer effects, and can be used for osteoporosis research .

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 .

Bazedoxifene Maximum Cited Publications 10 Publications Verification TSE-424	Estrogen Receptor/ERR	Cancer
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .

Bazedoxifene acetate Maximum Cited Publications 10 Publications Verification TSE-424 acetate	Estrogen Receptor/ERR	Cancer
Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .

Bazedoxifene hydrochloride TSE-424 hydrochloride	Estrogen Receptor/ERR	Cancer
Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer .

Delphinidin 3-glucoside chloride Delphinidin 3-O-glucoside chloride; Delphinidin 3-O-β-glucoside chloride	EGFR Apoptosis Akt	Cardiovascular Disease Cancer
Delphinidin 3-glucoside chloride (Delphinidin 3-O-glucoside chloride) is an active anthocyanin found in Hibiscus sabdariffa extract. Delphinidin 3-glucoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL) . Delphinidin 3-glucoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC₅₀ of 9.7 μM . Delphinidin-3-O-glucoside chloride inhibits EGFR with an IC₅₀ of 2.37 µM . Delphinidin 3-glucoside chloride exhibits antitumor effects through pAKT/IRF1/HOTAIR pathway. Delphinidin 3-glucoside chloride exhibits efficacy against oxidative stress, inhibits platelet activation and endothelial dysfunction .

Cat. No.	Product Name	Category	Target	Chemical Structure

Ferutinin	Infection Classification of Application Fields Terpenoids Sesquiterpenes Source classification Thymus quinquecostatus Cêlak. Plants Umbelliferae Disease Research Fields Endocrinology Cancer	Estrogen Receptor/ERR Apoptosis
Ferutinin, a natural terpenoid compound, is an estrogen receptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC₅₀s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca ²⁺-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities .

Estriol 3 Publications Verification Oestriol	Structural Classification Monophenols Immune System Disorder Classification of Application Fields Source classification Disease markers Phenols Endocrine diseases Endogenous metabolite Disease Research Fields Steroids Cancer	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 .

Delphinidin 3-glucoside chloride Delphinidin 3-O-glucoside chloride; Delphinidin 3-O-β-glucoside chloride	Malvaceae Structural Classification Anthocyans Flavonoids Microorganisms Classification of Application Fields Hibiscus sabdariffa Linn. Source classification Plants Disease Research Fields Cancer	EGFR Apoptosis Akt
Delphinidin 3-glucoside chloride (Delphinidin 3-O-glucoside chloride) is an active anthocyanin found in Hibiscus sabdariffa extract. Delphinidin 3-glucoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL) . Delphinidin 3-glucoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC₅₀ of 9.7 μM . Delphinidin-3-O-glucoside chloride inhibits EGFR with an IC₅₀ of 2.37 µM . Delphinidin 3-glucoside chloride exhibits antitumor effects through pAKT/IRF1/HOTAIR pathway. Delphinidin 3-glucoside chloride exhibits efficacy against oxidative stress, inhibits platelet activation and endothelial dysfunction .

Cat. No.	Product Name	Chemical Structure

Ospemifene D4
Ospemifene-d₄ is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects[1][2].

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