2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Estrogen Receptor/ERR
  5. Estrogen Receptor/ERR Modulator

Estrogen Receptor/ERR Modulator

Estrogen Receptor/ERR Isoform Comparison

Estrogen Receptor/ERR Modulators (95):

Cat. No. Product Name Effect Purity
  • HY-131586
    3,7-Dihydroxyflavone
    		Modulator
    3,7-Dihydroxyflavone (Resogalangin) is a flavonoid phytoestrogen, which can be isolated from Adenophora species. 3,7-Dihydroxyflavone is a modulator of estrogen receptors and an inhibitor of human progesterone metabolizing enzyme AKR1C1 and fungal 17β-hydroxysteroid dehydrogenase and a redox inhibitor (IC50=0.6 and 6.0 μM, respectively). 3,7-Dihydroxyflavone is a fluorescent binding substrate for human serum albumin (HSA) with excitation wavelengths of 370 nm (pH 7.4) and 350 nm (pH 3.5), respectively, and emission wavelength of 515 nm.
  • HY-B0723S
    Ospemifene-d4
    		Modulator
    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].
  • HY-135582S
    Raloxifene 4'-glucuronide-d4
    		Modulator
    Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-126109
    (±)-8-Prenylnaringenin
    		Modulator
    (±)-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-107045
    CHF 4227 free base
    		Modulator
    CHF 4227 free base is an orally active and selective estrogen receptor modulator (SERM) with high affinity to the human estrogen receptor-α and -β (Ki values of 0.017 nM and 0.099 nM, respectively).
  • HY-B0005S1
    Toremifene-d6 hydrochloride
    		Modulator
    Toremifene-d6 (Z-Toremifene-d6) hydrochloride is deuterium labeled Toremifene. Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
  • HY-119088
    Estrogen receptor modulator 12
    		Modulator
    Estrogen receptor modulator 12 (compound 1a-(R)) is a selective estrogen receptor modulator with estrogen agonist and antagonist activities in in vivo models. Estrogen receptor modulator 12 exhibits antagonist effects on the uterus and estrogen agonist activities on bone, plasma lipids, hot flashes, and vagina in in vivo models, and is a potential compound for suppressing postmenopausal symptoms.
  • HY-164726
    Estrogen receptor modulator 11
    		Modulator
    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-A0031S
    Bazedoxifene-d4
    		Modulator
    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-16950AR
    (E/Z)-4-Hydroxytamoxifen (Standard)
    		Modulator
    (E/Z)-4-Hydroxytamoxifen (Standard) is the analytical standard of (E/Z)-4-Hydroxytamoxifen. This product is intended for research and analytical applications. (E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is an estrogen receptor modulator.
  • HY-13556
    Arzoxifene
    		Modulator
    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.
  • HY-N3755R
    Dihydroresveratrol (Standard)
    		Modulator
    Clofarabine (Standard) is the analytical standard of Clofarabine. This product is intended for research and analytical applications. Clofarabine, a nucleoside analogue for research of cancer, is a potent inhibitor of ribonucleotide reductase (IC50=65 nM) by binding to the allosteric site on the regulatory subunit.
  • HY-122359
    Levormeloxifene
    		Modulator
    Levormeloxifene (L-Centchroman) is a selective estrogen receptor modulator (SERM), which prevents and ameliorates postmenopausal osteoporosis. Levormeloxifene causes multiple adverse gynecological effects.
  • HY-135582S1
    Raloxifene 4'-glucuronide-d4 lithium
    		Modulator
    Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
  • HY-135590
    Raloxifene 4-Monomethyl Ether
    		Modulator
    Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 1 μM and a pIC50 of 6.
  • HY-107043
    7β-Hydroxy-epi-androsterone
    		Modulator
    7β-Hydroxy-epi-androsterone (7β-Hydroxy-EpiA) can bind to ERβ and has anti-inflammatory and neuroprotective properties. 7β-Hydroxy-epi-androsterone is an endogenous androgenic derivative of dehydroepiandrosterone.
  • HY-127133
    Methylpiperidino pyrazole
    		Modulator
    Methylpiperidino pyrazole (MPP) is a potent and selective ER (estrogen receptor) modulator. Methylpiperidino pyrazole induces significant apoptosis in the endometrial cancer and oLE cell lines. Methylpiperidino pyrazole reverses the the positive effects of beta-estradiol. Methylpiperidino pyrazole has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
  • HY-121149B
    (E/Z)-Droloxifene
    		Modulator
    (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.
  • HY-13738S3
    Raloxifene-d10
    		Modulator
    Raloxifene-d10 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[1].
  • HY-122359A
    rel-Levormeloxifene
    		Modulator
    rel-Levormeloxifene (rel-L-Centchroman) is the relative configuration of Levormeloxifene (HY-122359). rel-Levormeloxifene is a selective estrogen receptor modulator (SERM). rel-Levormeloxifene inhibits proliferation of leukemia cells with IC50 about 7 μM, arrests cell cycle at G0/G1 phase, and induces apoptosis. rel-Levormeloxifene induces differentation of myelogenesis leukemia, and enhances ROS production in K562 cells.