Estrogen Receptor/ERR Modulator

Raloxifene-d₄ (hydrochloride) 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.

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.

Trioxifene mesylate (LY133314) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC₅₀ of 203.49 nM and K_i of 20.84 nM. Trioxifene mesylate binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene mesylate can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma.

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.

Trioxifene (LY133314 free base) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC₅₀ of 203.49 nM and K_i of 20.84 nM. Trioxifene binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma.

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.

HMR-3339 is a new selective estrogen receptor modulator. HMR-3339 reduces total cholesterol, low-density lipoprotein cholesterol, and homocysteine. HMR-3339 corrects bone alterations induced by ovariectomy.

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 (K_i values of 0.017 nM and 0.099 nM, respectively).

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.