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antiestrogens

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (3) Autophagy (3) Calcium Channel (1) Drug Metabolite (2) Endogenous Metabolite (2) Estrogen Receptor/ERR (16) Isotope-Labeled Compounds (1) PKC (2)
By Research Areas:	Cancer (16) Endocrinology (5) Inflammation/Immunology (1) Metabolic Disease (1)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-125263

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 .

HY-125263B

(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 .

HY-129099A

N-Desmethyltamoxifen hydrochloride	PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite	Cancer
N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation .

HY-117153

GW7604	Estrogen Receptor/ERR	Cancer
GW7604 is an antiestrogen. GW7604 is the metabolite of GW5638, which is a high affinity estrogen receptor (ER) antagonist .

HY-118633

Ethamoxytriphetol MER-25	Others	Endocrinology
Ethamoxytriphetol (MER-25) is a nonsteroidal antiestrogen .

HY-145556

Bexirestrant	Estrogen Receptor/ERR	Cancer
Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic .

HY-W926789

(E)-GW7604	Estrogen Receptor/ERR	Metabolic Disease Cancer
(E)-GW7604 is the (E)-isomer of GW7604, an antiestrogen and a metabolite of GW5638 (HY-112746), which is a high-affinity estrogen receptor (ER) antagonist .

HY-129099

N-Desmethyltamoxifen	PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite	Cancer
N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation .

HY-118242

RU 45144	Others	Others
RU 45144 is an anti-estrogen compound that has the activity of antagonizing the binding of estrogen receptors to calmodulin. RU 45144 can inhibit the binding of estrogen receptors to calmodulin, and its effect is similar to that of tamoxifen. Its anti-estrogen effect may be related to specific side chains in the molecular structure, and the steroid skeleton may be involved in its anti-proliferative activity.

HY-103452

RU58668	Estrogen Receptor/ERR	Endocrinology
RU58668 is a steroidal antiestrogen that can be used as a potent antiproliferative agent on MCF-7 cells. RU58668 has the potential for the breast cancer research .

HY-W150752

Triphenylethylene	Estrogen Receptor/ERR Calcium Channel	Endocrinology
Triphenylethylene is an aromatic hydrocarbon that possesses weak estrogenic activity. Triphenylethylene antiestrogens relax duodenal intestinal muscle via a mechanism that involves inhibition of L-type Ca ²⁺ channels but not activation of K ⁺ channels .

HY-117649

RU-39411	Others	Cancer
RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .

HY-N3316

Martynoside	Others
Martynoside protects ex vivo bone marrow cells from 5-fluorouracil (5-FU)-induced cell death and inflammation response by down-regulating the TNF signaling pathway .Martynoside is a potent antiestrogen in MCF-7 cells, increasing IGFBP3 levels

HY-106056

Zindoxifene D 16726	Others	Cancer
Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .

HY-13636

Fulvestrant Maximum Cited Publications 83 Publications Verification ICI 182780; ZD 9238; ZM 182780	Estrogen Receptor/ERR Autophagy Apoptosis	Cancer
Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC₅₀ of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC₅₀ of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .

HY-117038

Anordiol	Others	Endocrinology
Anordiol is an antiestrogenic compound with weak estrogenic activity. It can reduce the parameters of uterine growth (including uterine wet weight, soluble protein content, and DNA content) induced by estradiol in rats and can also regulate the estrous cycle in rats. Anordiol holds potential application value in the research of antiestrogen-related diseases .

HY-148789

Palazestrant OP-1250	Estrogen Receptor/ERR	Inflammation/Immunology Cancer
Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC₅₀ value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC₅₀ value of 1.4-1.6 nM. Palazestrant can inhibit ER ⁺/HER2 ⁺ cancer .

HY-13636S

Fulvestrant-d3 ICI 182780-d₃; ZD 9238-d₃; ZM 182780-d₃	Isotope-Labeled Compounds Estrogen Receptor/ERR Autophagy Apoptosis	Cancer
Fulvestrant-d₃ is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].

HY-13636R

Fulvestrant (Standard) Maximum Cited Publications 83 Publications Verification ICI 182780(Standard); ZD 9238(Standard); ZM 182780 (Standard)	Estrogen Receptor/ERR Autophagy Apoptosis	Cancer
Fulvestrant (Standard) is the analytical standard of Fulvestrant. This product is intended for research and analytical applications. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC₅₀ of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC₅₀ of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .

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-13558

Atamestane SH 489	Estrogen Receptor/ERR	Endocrinology
Atamestane (SH 489) is a specific aromatase inhibitor, which selectively blocks the estrogen biosynthesis resulting from the aromatization of androstenedione and testosterone. Atamestane is a competitive and irreversible inhibitor of estrogen biosynthesis. Atamestane can be used for the research of benign prostatic hyperplasia (BPH) .

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-145341

GNE-149	Estrogen Receptor/ERR	Cancer
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC₅₀=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-129099A

N-Desmethyltamoxifen hydrochloride	Structural Classification Alkaloids Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields Cancer	PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite
N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation .

HY-N3316

Martynoside	Simple Phenylpropanols Labiatae Source classification Phenols Polyphenols Ligularia muliensis Hand.-Mazz. Phenylpropanoids Plants	Others
Martynoside protects ex vivo bone marrow cells from 5-fluorouracil (5-FU)-induced cell death and inflammation response by down-regulating the TNF signaling pathway .Martynoside is a potent antiestrogen in MCF-7 cells, increasing IGFBP3 levels

HY-129099

N-Desmethyltamoxifen	Structural Classification Alkaloids Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields Cancer	PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite
N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation .

Cat. No.	Product Name	Chemical Structure

HY-13636S

Fulvestrant-d3
Fulvestrant-d₃ is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].

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antiestrogens

Inhibitors & Agonists

NaturalProducts

Isotope-Labeled Compounds

Natural
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