1. Signaling Pathways
  2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR

Estrogen Receptor/ERR

Estrogen receptors are a group of proteins found inside cells. They are receptors that are activated by the hormone estrogen (17β-estradiol). Two classes of estrogen receptor exist: ER, which is a member of the nuclear hormone family of intracellular receptors, and GPER (GPR30), which is a member of the rhodopsin-like family of G protein-coupled receptors. The ER's helix 12 domain plays a crucial role in determining interactions with coactivators and corepressors and, therefore, the respective agonist or antagonist effect of the ligand. Different ligands may differ in their affinity for alpha and beta isoforms of the estrogen receptor: estradiol binds equally well to both receptors, estrone, and raloxifene bind preferentially to the alpha receptor, estriol, and genistein to the beta receptor. Estrogen and its receptors are essential for sexual development and reproductive function, but also play a role in other tissues such as bone. Estrogen receptors are also involved in pathological processes including breast cancer, endometrial cancer, and osteoporosis. Alternative promoter usage and alternative splicing result in dozens of transcript variants, but the full-length nature of many of these variants has not been determined.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-116939
    (E)-Broparestrol
    Activator
    (E)-Broparestrol is a biologically active tetrasubstituted olefin, which is used as an estrogen in dermatology.
    (E)-Broparestrol
  • HY-B2245R
    Estradiol dipropionate (Standard)
    Agonist
    Estradiol dipropionate (Standard) is the analytical standard of Estradiol dipropionate. This product is intended for research and analytical applications. Estradiol dipropionate is a combined estrogen-progesterone, acts as an estrogen and progesterone agonist.
    Estradiol dipropionate (Standard)
  • HY-10426R
    XCT790 (Standard)
    Antagonist
    XCT790 (Standard) is the analytical standard of XCT790 (HY-10426). This product is intended for research and analytical applications. XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.
    XCT790 (Standard)
  • HY-100583AR
    (±)-Equol (Standard)
    (±)-Equol (Standard) is the analytical standard of (±)-Equol. This product is intended for research and analytical applications. (±)-Equol is the racemate of equol. (±)-equol exhibits EC50s of 200 and 74 nM for human ERα and ERβ, respectively. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.
    (±)-Equol (Standard)
  • HY-W615671
    4,4'-(Cyclohexylidenemethylene)diphenol
    Ligand
    4,4'-(Cyclohexylidenemethylene)diphenol (Compound 2) is a symmetric cyclic nonsteroidal estrogen. 4,4'-(Cyclohexylidenemethylene)diphenol has high binding affinity for estrogen receptors ERα and ERβ.
    4,4'-(Cyclohexylidenemethylene)diphenol
  • HY-103454R
    MPP dihydrochloride (Standard)
    Modulator
    MPP dihydrochloride (Standard) is the analytical standard of MPP dihydrochloride (HY-103454). This product is intended for research and analytical applications. MPP dihydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP dihydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP dihydrochloride reverses the positive effects of beta-estradiol. MPP dihydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
    MPP dihydrochloride (Standard)
  • HY-100689R
    Propyl pyrazole triol (Standard)
    Agonist
    Propyl pyrazole triol (Standard) is the analytical standard of Propyl pyrazole triol. This product is intended for research and analytical applications. Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).
    Propyl pyrazole triol (Standard)
  • HY-N15336
    Tschimganin
    Tschimganin is an ester of terpenoid acids with estrogen activity, which is found in F. tschimganica. Tschimganin can increase the growth of uterus of immature rats.
    Tschimganin
  • HY-W020788R
    Benoxacor (Standard)
    Activator
    Benoxacor (Standard) is the analytical standard of Benoxacor. This product is intended for research and analytical applications. Benoxacor (CGA 154281) is a herbicide safener and xenobiotic metabolism regulator. Benoxacor protects maize from the toxicity of metolachlor mainly by inducing detoxifying enzymes such as Glutathione S-transferase. Benoxacor also activates FXR, PXR and ERRα, and inhibits aromatase (aromatase). However, Benoxacor exhibits potential subacute oral toxicity and a high risk of hepatotoxicity in animal models. Benoxacor induces reactive oxygen species accumulation, interferes with embryonic heart development, and causes increased liver and kidney weights as well as alterations in gut microbiota in mice. Benoxacor can be used in studies related to hepatic steatosis, infertility, breast cancer and developmental toxicity.
    Benoxacor (Standard)
  • HY-103450R
    G36 (Standard)
    Antagonist
    G36 (Standard) is the analytical standard of G36 (HY-103450). This product is intended for research and analytical applications. G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer.
    G36 (Standard)
  • HY-A0031R
    Bazedoxifene (Standard)
    Modulator
    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 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.
    Bazedoxifene (Standard)
  • HY-N2168R
    Pinoresinol 4-O-β-D-glucopyranoside (Standard)
    Pinoresinol 4-O-β-D-glucopyranoside (Standard) is the analytical standard of Pinoresinol 4-O-β-D-glucopyranoside (HY-N2168). This product is intended for research and analytical applications. Pinoresinol 4-O-β-D-glucopyranoside is an orally active α-glucosidase inhibitor, with an IC50 of 48.13 μg/mL. Pinoresinol 4-O-β-D-glucopyranoside binds to estrogen receptors. Pinoresinol 4-O-β-D-glucopyranoside inhibits phosphodiesterase. Pinoresinol 4-O-β-D-glucopyranoside exhibits various activities such as antioxidant, anti-inflammatory, anti-hyperglycemic, hepatoprotective and anti-epileptic effects.
    Pinoresinol 4-O-β-D-glucopyranoside (Standard)
  • HY-N15473
    Isopaucifloral F
    Agonist
    Isopaucifloral F ((±)-Isopaucifloral F) is a Resveratrol (HY-16561)-derived sesquiterpenes. Isopaucifloral F is an orally active ERβ agonist (EC50: 46.96 μM). Isopaucifloral F has antiosteoporosis activity. LD50 in rats: > 5 mg/kg.
    Isopaucifloral F
  • HY-118861AS1
    Clomiphene-d5 citrate
    Antagonist
    Clomiphene-d5 (citrate) is the deuterium labeled Enclomiphene citrate. Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property.
    Clomiphene-d<sub>5</sub> citrate
  • HY-W354544
    (Rac)-Hexestrol
    Agonist
    (Rac)-Hexestrol is the racemic form of Hexestrol (HY-B1662). Hexestrol is a synthetic non-steroidal estrogen. (Rac)-Hexestrol usually appears in deuterated form and is used as an internal standard for precise quantitative analysis in analytical chemistry.
    (Rac)-Hexestrol
  • HY-B0141S6
    Estradiol-d2-1
    Agonist
    Estradiol-d2-1 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
    Estradiol-d<sub>2</sub>-1
  • HY-B0005R
    Toremifene citrate (Standard)
    Modulator
    Toremifene (citrate) (Standard) is the analytical standard of Toremifene (citrate). This product is intended for research and analytical applications. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
    Toremifene citrate (Standard)
  • HY-103449R
    G15 (Standard)
    Antagonist
    G15 (Standard) is the analytical standard of G15 (HY-103449). This product is intended for research and analytical applications. G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.
    G15 (Standard)
  • HY-108293R
    Promestriene (Standard)
    Agonist
    Promestriene (Standard) is the analytical standard of Promestriene. This product is intended for research and analytical applications. Promestriene is a synthetic diethyl-ether of estradiol and a locally effective estrogen. Promestriene has an efficient action on vaginal atrophy while it is minimally absorbed.
    Promestriene (Standard)
  • HY-163712
    17-Epiestriol
    Agonist
    17-Epiestriol is an estrogen metabolite and a selective estrogen receptor (ER) β agonist. 17-epiestriol inhibits the mRNA and protein expression of the vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα). 17-epiestriol also inhibits TNFα-induced VCAM-1 expression and prevents NF-κB migration to the nucleus. 17-Epiestriol also induces the mRNA and protein expression of endothelial nitric oxide synthase.
    17-Epiestriol
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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