Estrogen Receptor/ERR Modulator

R4K1 is a cell-permeable stapled peptide. R4K1 binds to the estrogen receptor (ER) α with high affinity and inhibits its interaction with coactivators. R4K1 can enter breast cancer cells to regulate gene transcription and inhibit cell proliferation. R4K1 can be used in the study of cancer.

Estrogen receptor modulator 7 is a potent estrogen receptor modulator. Estrogen receptor modulator 7 can be used in research of cancer.

Toremifene-d₆ is deuterium labeled Toremifene. Toremifene (Z-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.

4'-Hydroxytamoxifen (Standard) is the analytical standard of 4'-Hydroxytamoxifen. This product is intended for research and analytical applications. 4'-Hydroxytamoxifen is a metabolite of Tamoxifen. 4'-Hydroxytamoxifen shows higher affinity for the ER than Tamoxifen. 4'-Hydroxytamoxifen induces a non-apoptotic cytotoxic effect in human endometrial adenocarcinoma cells.

Raloxifene 6-glucuronide-d₄ (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC₅₀ of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.

Genistin (Standard) is the analytical standard of Genistin. This product is intended for research and analytical applications. Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway.

Levormeloxifene (fumarate) is a stable salt form of Levormeloxifene. Levormeloxifene (fumarate) is an estrogen receptor modulator that plays an important role in prevention of postmenopausal bone loss.

(Z)-Norendoxifen is an aromatase inhibitor and estrogen receptor modulator. The IC₅₀ value of (Z)-Norendoxifen against aromatase is 102 nM. The EC₅₀ values of (Z)-Norendoxifen for ER-α and ER-β are 27.0 nM and 35.2 nM, respectively. (Z)-Norendoxifen can be used in breast cancer research.

Ethamoxytriphetol (MER-25) is a nonsteroidal antiestrogen.

SR-16157 (NSC 732011; HLX-801) is a dual-action steroid sulfatase (STS) inhibitor (IC₅₀ = 0.1 uM) and selective ERα modulator. SR-16157 exhibits STS inhibitory and anti-estrogenic effects in breast cancer cells. SR-16157 may be used in breast cancer research.

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.

Psidial A is an epimer of sesquiterpenoid-diphenylmethane meroterpenoid. Psidial A may act as a selective estrogen receptors modulator. Psidial A also has potential for anticancer research.

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.

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.

Icariside D1 (Compound 9) is a flavonoid glycoside compound with antioxidant and anti-inflammatory activities, which is found in plants such as Epimedium. Icariside D1 is also a regulator of estrogen receptors. Icariside D1 is promising for research of osteoporosis, male infertility and female reproductive dysfunction and cancers.

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.

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.

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.

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].

(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 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.