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Anti-estrogenic

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50

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11

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8

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Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 .
    (Rac)-Acolbifene
  • 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 .
    Quassin
  • 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).
    Endoxifen Z-isomer hydrochloride
  • 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.
    OP-1074
  • 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
    7-Hydroxyflavanone
  • 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.
    (R)-OP-1074
  • 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 .
    Guajadial
  • HY-148225
    Fulvestrant 3-β-D-Glucuronide

    		Drug Metabolite 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 .
    Fulvestrant 3-β-D-Glucuronide
  • 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 .
    AhR modulator-1
  • 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 .
    Quassin (Standard)
  • 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 .
    Octinoxate
  • HY-18719
    Endoxifen (Z-isomer)
    3 Publications Verification

    		 Estrogen Receptor/ERR Potassium Channel Cancer
    Endoxifen Z-isomer is an oral active Tamoxifen (HY-13757A) 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 .
    Endoxifen (Z-isomer)
  • HY-B1234S
    Octinoxate-13C,d3

    		Cytochrome P450 Thyroid Hormone Receptor Androgen Receptor Estrogen Receptor/ERR Isotope-Labeled Compounds Metabolic Disease Endocrinology
    Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). 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 .
    Octinoxate-13C,d3
  • 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) .
    Permethrin
  • HY-B1095
    Chlormadinone acetate
    1 Publications Verification

    		 Progesterone Receptor Endocrinology
    Chlormadinone acetate is a steroidal progestin, with antiandrogen and antiestrogenic effects.
    Chlormadinone acetate
  • HY-118242
    RU 45144

    		Estrogen Receptor/ERR Calmodulin 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.
    RU 45144
  • HY-113251
    2-Hydroxyestrone

    Catecholestrone

    		 Endogenous Metabolite Estrogen Receptor/ERR Endocrinology Cancer
    2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic .
    2-Hydroxyestrone
  • HY-123664
    Trioxifene mesylate

    LY133314

    		 Estrogen Receptor/ERR Endocrinology
    Trioxifene mesylate (LY133314) is an antiestrogenic compound. Trioxifene mesylate elicits mixed agonist-antagonist actions on estrogen target tissues .
    Trioxifene mesylate
  • HY-B1095S2
    Chlormadinone acetate-d3

    		Isotope-Labeled Compounds Progesterone Receptor Endocrinology
    Chlormadinone acetate-d3 is the deuterium labeled Chlormadinone acetate. Chlormadinone acetate is a steroidal progestin, with antiandrogen and antiestrogenic effects[1].
    Chlormadinone acetate-d3
  • HY-122411
    Panomifene

    EGIS 5650; GYKI-13504

    		 Estrogen Receptor/ERR Cancer
    Panomifene (EGIS 5650) is a tamoxifen (HY-13757A) analog with an antiestrogenic activity. Panomifene can be used in the research of breast cancer .
    Panomifene
  • HY-N1507
    Tracheloside

    		Estrogen Receptor/ERR Cancer
    Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing .
    Tracheloside
  • HY-121441
    Fispemifene

    		Estrogen Receptor/ERR Inflammation/Immunology
    Fispemifene, an orally active selective estrogen receptor modulator with anti-inflammatory and antiestrogenic action, attenuates glandular inflammation in an animal model of chronic nonbacterial prostatitis .
    Fispemifene
  • HY-18719D
    Endoxifen (E-isomer)

    E-Endoxifen

    		 Estrogen Receptor/ERR Cancer
    Endoxifen E-isomer (E-Endoxifen), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer agent substance. Endoxifen E-isomer exhibits antiestrogenic effects .
    Endoxifen (E-isomer)
  • HY-18719C
    Endoxifen E-isomer hydrochloride

    E-Endoxifen hydrochloride

    		 Estrogen Receptor/ERR Cancer
    Endoxifen E-isomer hydrochloride (E-Endoxifen hydrochloride), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer agent substance. Endoxifen E-isomer hydrochloride exhibits antiestrogenic effects .
    Endoxifen E-isomer hydrochloride
  • HY-N3257
    Millewanin G

    		Estrogen Receptor/ERR Endocrinology
    Millewanin G is a prenylated isoflavonoid with antiestrogenic activity (IC50=29 μM). Millewanin G can be isolated from the leaves of M. pachycarpa cultivated in Japan .
    Millewanin G
  • HY-10830A
    PBPE hydrochloride

    		Estrogen Receptor/ERR Cancer
    PBPE hydrochloride is a derivative of tamoxifen (HY-13757A) and a selective ligand for the anti-estrogen binding site (AEBS), the binding affinities (Ki) of PBPE hydrochloride and MBPE to AEBS are 8.79 and 17.57 nM, respectively .
    PBPE hydrochloride
  • HY-105634
    Nomegestrol

    		Progesterone Receptor Endocrinology Cancer
    Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
    Nomegestrol
  • HY-N11787
    Cimicifuga racemosa extract

    		Estrogen Receptor/ERR Metabolic Disease
    Cimicifuga racemosa extract is a herbal remedy with antiestrogenic properties found in the plant Cimicifuga racemosa, commonly used to alleviate menopausal symptoms and relieve symptoms such as hot flashes and night sweats .
    Cimicifuga racemosa extract
  • HY-113251S
    2-Hydroxyestrone-d4

    Catecholestrone-d4

    		 Isotope-Labeled Compounds Endogenous Metabolite Estrogen Receptor/ERR Endocrinology Cancer
    2-Hydroxyestrone-d4 is the deuterium labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic[1][2].
    2-Hydroxyestrone-d4
  • HY-113251S1
    2-Hydroxyestrone-13C6

    Catecholestrone-13C6

    		 Isotope-Labeled Compounds Endogenous Metabolite Estrogen Receptor/ERR Endocrinology Cancer
    2-Hydroxyestrone- 13C6 is the 13C-labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic[1][2].
    2-Hydroxyestrone-13C6
  • HY-B2158
    Chlorotrianisene

    		Estrogen Receptor/ERR COX Cardiovascular Disease Endocrinology
    Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood .
    Chlorotrianisene
  • HY-N1507R
    Tracheloside (Standard)

    		Estrogen Receptor/ERR Cancer
    Tracheloside (Standard) is the analytical standard of Tracheloside. This product is intended for research and analytical applications. Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing .
    Tracheloside (Standard)
  • HY-B1617A
    Zuclomiphene citrate
    1 Publications Verification

    		 Estrogen Receptor/ERR Metabolic Disease Endocrinology
    Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent .
    Zuclomiphene citrate
  • HY-147813
    HIF-1α-IN-3

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-3 (Compound (S)-3f) is a hypoxia-selective HIF-1α inhibitor. HIF-1α-IN-3 shows strong antiestrogenic potency .
    HIF-1α-IN-3
  • HY-121149
    Droloxifene
    1 Publications Verification

    3-Hydroxytamoxifen

    		 Estrogen Receptor/ERR Apoptosis Cancer
    Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
    Droloxifene
  • HY-13556
    Arzoxifene

    LY353381; SERM III

    		 Estrogen Receptor/ERR Metabolic Disease Cancer
    Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile .
    Arzoxifene
  • HY-106056
    Zindoxifene

    D 16726

    		 Estrogen Receptor/ERR 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 .
    Zindoxifene
  • HY-B1617AS
    Zuclomiphene-d4 citrate

    		Estrogen Receptor/ERR Metabolic Disease Endocrinology
    Zuclomiphene-d4 (citrate) is a deuterium labeled Zuclomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent[1][2][3][4].
    Zuclomiphene-d4 citrate
  • HY-B2158S
    Chlorotrianisene-d9

    		Estrogen Receptor/ERR COX Cardiovascular Disease Endocrinology
    Chlorotrianisene-d9 is the deuterium labeled Chlorotrianisene. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood[1][2][3].
    Chlorotrianisene-d9
  • HY-119437
    FLTX1
    2 Publications Verification

    		 Estrogen Receptor/ERR Cancer
    FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus .
    FLTX1
  • HY-117038
    Anordiol

    		Estrogen Receptor/ERR 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 .
    Anordiol
  • HY-B2158R
    Chlorotrianisene (Standard)

    		Estrogen Receptor/ERR COX Cardiovascular Disease Endocrinology
    Chlorotrianisene (Standard) is the analytical standard of Chlorotrianisene. This product is intended for research and analytical applications. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood .
    Chlorotrianisene (Standard)
  • HY-B1617AS2
    Zuclomiphene d10 Citrate salt

    		Isotope-Labeled Compounds Estrogen Receptor/ERR Metabolic Disease Endocrinology
    Zuclomiphene d10 Citrate salt is deuterium labeled Zuclomiphene (citrate). Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent .
    Zuclomiphene d10 Citrate salt
  • HY-B1617AS1
    Zuclomiphene-d5 citrate

    		Estrogen Receptor/ERR Endocrinology
    Zuclomiphene-d5 (citrate) is the deuterium labeled Zuclomiphene citrate[1]. Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent[2][3][4][5].
    Zuclomiphene-d5 citrate
  • 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 (Ki: 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 .
    LY2066948
  • 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 .
    Acolbifene hydrochloride
  • 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 .
    EM-800
  • 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 .
    RU-39411
  • HY-16950A
    (E/Z)-4-Hydroxytamoxifen
    1 Publications Verification

    Afimoxifene; 4-OHT

    		 Estrogen Receptor/ERR Adhesion G Protein-coupled Receptors (AGPCRs) Drug Metabolite Metabolic Disease Cancer
    (E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity .
    (E/Z)-4-Hydroxytamoxifen
  • HY-121149B
    (E/Z)-Droloxifene

    (E/Z)-3-Hydroxytamoxifen

    		 Estrogen Receptor/ERR Apoptosis Cancer
    (E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity .
    (E/Z)-Droloxifene

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