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Results for "

ERα modulator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Caspase (1) Cytochrome P450 (1) Endogenous Metabolite (2) Estrogen Receptor/ERR (23) Isotope-Labeled Compounds (4) NO Synthase (2) Reference Standards (2) Steroid Sulfatase (1)
By Research Areas:	Cancer (21) Cardiovascular Disease (2) Endocrinology (2) Metabolic Disease (1) Neurological Disease (2)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-A0036

Bazedoxifene acetate Maximum Cited Publications 16 Publications Verification TSE-424 acetate	Estrogen Receptor/ERR	Cancer
Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal *selective estrogen receptor modulator* (SERM), with IC₅₀*s 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 .

HY-A0031

Bazedoxifene Maximum Cited Publications 16 Publications Verification TSE-424	Estrogen Receptor/ERR	Neurological Disease Cancer
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal *selective estrogen receptor modulator* (SERM), with IC₅₀*s 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 .

HY-B0723

Ospemifene 2 Publications Verification FC-1271a	Estrogen Receptor/ERR Caspase	Neurological Disease Endocrinology Cancer
Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with K_i values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer .

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-126109

(±)-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 .

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-A0036D

Bazedoxifene acetate-D TSE-424 acetate-D	Estrogen Receptor/ERR	Cancer
Bazedoxifene (acetate)-D (TSE-424 (acetate)-D) is the D-crystal form compound of Bazedoxifene acetate (HY-A0036). Bazedoxifene acetate is an orally active, nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively .

HY-A0031A

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 IC₅₀*s 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 .

HY-A0036R

Bazedoxifene acetate (Standard) TSE-424 acetate (Standard)	Reference Standards Estrogen Receptor/ERR	Cancer
Bazedoxifene (acetate) (Standard) is the analytical standard of Bazedoxifene (acetate). This product is intended for research and analytical applications. Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal *selective estrogen receptor modulator* (SERM), with IC₅₀*s 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 .

HY-16023

Acolbifene hydrochloride 2 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 .

HY-123773

SR-16157 NSC 732011; HLX-801	Steroid Sulfatase Estrogen Receptor/ERR	Cancer
SR-16157 (NSC 732011; HLX-801) is a dual-action steroid sulfatase (STS) inhibitor (IC₅₀ = 0.1 uM) and selective *ERα* modulator. SR-16157 exhibits STS inhibitory and anti-estrogenic effects in breast cancer cells. SR-16157 may be used in breast cancer research .

HY-A0031R

Bazedoxifene (Standard) TSE-424 (Standard)	Reference Standards Estrogen Receptor/ERR	Cancer
Bazedoxifene (Standard) is the analytical standard of Bazedoxifene. This product is intended for research and analytical applications. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal *selective estrogen receptor modulator* (SERM), with IC₅₀*s 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 .

HY-123664

Trioxifene mesylate LY133314	Estrogen Receptor/ERR	Cancer
Trioxifene mesylate (LY133314) is an orally active and selective estrogen receptor (ER) modulator with human *ERα* IC₅₀ of 203.49 nM and K_i of 20.84 nM. Trioxifene mesylate binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene mesylate can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma .

HY-B0723S

Ospemifene-d4 FC-1271a-d₄	Isotope-Labeled Compounds 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 .

HY-B0723S2

Ospemifene-d5 FC-1271a-d₅	Isotope-Labeled Compounds Estrogen Receptor/ERR	Cancer
Ospemifene-d₅ (FC-1271a-d₅) is deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with K_is of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer .

HY-125091

LY2066948	Estrogen Receptor/ERR	Cancer
LY2066948 is a selective and orally active estrogen receptor modulator (SERM). LY2066948 has high affinity for estrogen receptors *ERα* and ERβ (K_i: 0.51 and 1.36 nM respectively) and shows potent antiestrogenic activity. LY2066948 blocks uterine weight gain induced by Ethynyl estradiol (HY-B0216) in immature rats. LY2066948 can be used for research of uterine fibroids and myomas .

HY-A0031S

Bazedoxifene-d4 TSE-424-d₄	Isotope-Labeled Compounds Estrogen Receptor/ERR	Cancer
Bazedoxifene-d₄ is deuterium labeled Bazedoxifene. 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[1][2].

HY-A0031S2

Bazedoxifene-d4 acetate TSE-424-d4 acetate	Estrogen Receptor/ERR	Cancer
Bazedoxifene-d₄ (acetate) is the deuterium labeled Bazedoxifene[1]. 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[2][3].

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-135529

Trioxifene LY133314 free base	Estrogen Receptor/ERR	Cancer
Trioxifene (LY133314 free base) is an orally active and selective estrogen receptor (ER) modulator with human *ERα* IC₅₀ of 203.49 nM and K_i of 20.84 nM. Trioxifene binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma .

HY-181345

OP-1690	Estrogen Receptor/ERR	Cancer
OP-1690 is a complete estrogen receptor (ERα) antagonist (CERAN), with pIC₅₀ values of 7.5 and 7.9 in alkaline phosphatase (AP) activity assay and TR-FRET assay, respectively. OP-1690 modulates receptor function by inducing ERα tetramerization, effectively induces ERα degradation, inhibits target gene transcription, but exhibits low antiproliferative potency. OP-1690 can be used for breast cancer 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 .

HY-182498

(Z)-Norendoxifen	Cytochrome P450 Estrogen Receptor/ERR	Cancer
(Z)-Norendoxifen is an aromatase inhibitor and estrogen receptor modulator. The IC₅₀ value of (Z)-Norendoxifen against aromatase is 102 nM. The EC₅₀ values of (Z)-Norendoxifen for *ER-α* and ER-β are 27.0 nM and 35.2 nM, respectively. (Z)-Norendoxifen can be used in breast cancer research .

Cat. No.	Product Name	Category	Target	Chemical Structure

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-126109

(±)-8-Prenylnaringenin	Structural Classification Flavonoids Humulus lupulus L. Flavonones Plants Moraceae Source Classification	Estrogen Receptor/ERR Apoptosis
(±)-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 .

Cat. No.	Product Name	Chemical Structure

HY-B0723S

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 .

HY-B0723S2

Ospemifene-d5
Ospemifene-d₅ (FC-1271a-d₅) is deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with K_is of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer .

HY-A0031S

Bazedoxifene-d4
Bazedoxifene-d₄ is deuterium labeled Bazedoxifene. 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[1][2].

Bazedoxifene-d4

Bazedoxifene-d₄ is deuterium labeled Bazedoxifene. 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[1][2].

HY-A0031S2

Bazedoxifene-d4 acetate
Bazedoxifene-d₄ (acetate) is the deuterium labeled Bazedoxifene[1]. 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[2][3].

Bazedoxifene-d4 acetate

Bazedoxifene-d₄ (acetate) is the deuterium labeled Bazedoxifene[1]. 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[2][3].

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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