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Anti-estrogen

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Estrogen Receptor/ERR (22) Androgen Receptor (1) Apoptosis (2) Aryl Hydrocarbon Receptor (1) Autophagy (2) Calcium Channel (1) Cytochrome P450 (2) Drug Metabolite (2) Endogenous Metabolite (2) Mitochondrial Metabolism (1) Na+/K+ ATPase (1) Parasite (3) PKC (2) Potassium Channel (2) Sodium Channel (1) Thyroid Hormone Receptor (1) VEGFR (1)
By Research Areas:	Cancer (21) Endocrinology (11) Infection (3) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (1)

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Targets Recommended: Estrogen Receptor/ERR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P3833A

Yp537 TFA Anti-estrogen TFA	Estrogen Receptor/ERR	Endocrinology
Yp537 TFA is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor .

HY-125263

OP-1074	Estrogen Receptor/ERR	Cancer
OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription with IC₅₀ values of 1.6 and 3.2 nM, respectively.

HY-125263B

(R)-OP-1074	Estrogen Receptor/ERR	Cancer
(R)-OP-1074 is an isomer of OP-1074 (HY-125263) and can serve as a control compound in experiments. OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription with IC₅₀ values of 1.6 and 3.2 nM, respectively.

HY-P3833

Yp537 Anti-estrogen	Estrogen Receptor/ERR	Endocrinology
Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor .

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-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-117649

RU-39411	Estrogen Receptor/ERR	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-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-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-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-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-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-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-18719A

Endoxifen Z-isomer hydrochloride 3 Publications Verification	Estrogen Receptor/ERR Potassium Channel	Cancer
Endoxifen Z-isomer hydrochloride is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα).

HY-N3981

Guajadial	Others	Cancer
Guajadial, a caryophyllene-based meroterpenoid, has anti-estrogenic and anticancer effect. Guajadial reverses multidrug resistance in cancer. Guajadial can be isolated from Psidium guajava leaves .

HY-W087008

7-Hydroxyflavanone	Cytochrome P450	Endocrinology Cancer
7-Hydroxyflavanone is a potent inhibitor of aromatase (CYP19) activity with the IC₅₀ of 65 μM. 7-Hydroxyflavanone exerts various biological effects, including anticarcinogenic, antioxidant and (anti-)estrogenic effects, and modula

HY-18719

Endoxifen (Z-isomer) 3 Publications Verification	Estrogen Receptor/ERR Potassium Channel	Cancer
Endoxifen Z-isomer is the most important Tamoxifen metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM.

HY-N1581

Quassin Nigakilactone D	Parasite	Infection Endocrinology
Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits *P. falciparum* with an IC₅₀ of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity .

HY-148225

Fulvestrant 3-β-D-Glucuronide	Others	Cancer
Fulvestrant 3-β-D-Glucuronide, a metabolite, is glucuronide and sulfate conjugates of Fulvestrant (HY-13636), a pure anti-estrogenic steroid. Fulvestrant 3-β-D-Glucuronide can be used for the research of breast cancer .

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-13636

Fulvestrant Maximum Cited Publications 86 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-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-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-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-N1581R

Quassin (Standard)	Parasite	Infection Endocrinology
Quassin (Standard) is the analytical standard of Quassin. This product is intended for research and analytical applications. Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC₅₀ of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity .

HY-135671

AhR modulator-1	Aryl Hydrocarbon Receptor VEGFR Estrogen Receptor/ERR	Endocrinology Cancer
AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus .

HY-13636R

Fulvestrant (Standard) Maximum Cited Publications 86 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-16023B

(Rac)-Acolbifene EM-343; (Rac)-EM-652	Estrogen Receptor/ERR	Cancer
(Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor?antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380 .

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-B0887

Permethrin 1 Publications Verification NRDC-143	Parasite Mitochondrial Metabolism Sodium Channel Na+/K+ ATPase	Infection Neurological Disease
Permethrin (NRDC-143) is an insecticide, acaricide and a high selectively inhibitor of the Mitochondrial complex I, found in sediment and water samples. Permethrin shows *estrogenic* in vivo and anti-estrogenic activity in vitro. Permethrin also acts as a neurotoxin affecting neuron membranes by prolonging Sodium channel activation. Permethrin decreases resistance to bacterial infections in medaka (Oryzias latipes) .

HY-B1234

Octinoxate Octyl methoxycinnamate	Androgen Receptor Estrogen Receptor/ERR Thyroid Hormone Receptor Cytochrome P450	Metabolic Disease Endocrinology
Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an *anti-estrogenic* and *anti-androgenic* effect in vitro and in vivo .

Yp537 TFA Anti-estrogen TFA	Estrogen Receptor/ERR	Endocrinology
Yp537 TFA is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor .

Yp537 Anti-estrogen	Estrogen Receptor/ERR	Endocrinology
Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor .

Quassin Nigakilactone D	Triterpenes Structural Classification Simaroubaceae Classification of Application Fields Terpenoids Source classification Plants Disease Research Fields Picrasma quassioides(D．Don)Benn． Endocrinology	Parasite
Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits *P. falciparum* with an IC₅₀ of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity .

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

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 .

Octinoxate Octyl methoxycinnamate	Structural Classification Natural Products other families Classification of Application Fields Source classification Other Diseases Cosmetic Research Plants Disease Research Fields	Androgen Receptor Estrogen Receptor/ERR Thyroid Hormone Receptor Cytochrome P450
Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an *anti-estrogenic* and *anti-androgenic* effect in vitro and in vivo .

Guajadial	Structural Classification Natural Products Source classification Psidium guajava Linn. Myrtaceae Plants	Others
Guajadial, a caryophyllene-based meroterpenoid, has anti-estrogenic and anticancer effect. Guajadial reverses multidrug resistance in cancer. Guajadial can be isolated from Psidium guajava leaves .

7-Hydroxyflavanone	Dalbergia cochinchinensis Monophenols Source classification Papilionaceae Phenols Plants Disease Research Fields Endocrinology Cancer	Cytochrome P450
7-Hydroxyflavanone is a potent inhibitor of aromatase (CYP19) activity with the IC₅₀ of 65 μM. 7-Hydroxyflavanone exerts various biological effects, including anticarcinogenic, antioxidant and (anti-)estrogenic effects, and modula

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 .

Quassin (Standard)	Triterpenes Structural Classification Simaroubaceae Terpenoids Source classification Plants Picrasma quassioides(D．Don)Benn．	Parasite
Quassin (Standard) is the analytical standard of Quassin. This product is intended for research and analytical applications. Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC₅₀ of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity .

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Anti-estrogen

Inhibitors & Agonists

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