Estrogen Receptor/ERR 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.

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.

Diptoindonesin G is a 2-arylbenzofuran derivative and a modulator of estrogen receptor and HSP90 middle domain. Diptoindonesin G exhibits strong cytotoxicity against mouse leukemia P-388 cells with an IC₅₀ of 13.2 μM. Diptoindonesin G has antitumor activity and can be used in the research of tumors such as breast cancer.

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.

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.

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.

Levormeloxifene (L-Centchroman) is a selective estrogen receptor modulator (SERM), which prevents and ameliorates postmenopausal osteoporosis. Levormeloxifene causes multiple adverse gynecological effects.

Zuclomiphene is a cis isomer of Clomiphene citrate (HY-B0463). Zuclomiphene is orally active and has an antiestrogenic effect. Zuclomiphene can reduce cholesterol levels. Zuclomiphene can be for the researches of endocrinology and metabolic disease.

Zuclomiphene d₁₀ Citrate salt is deuterium labeled Zuclomiphene citrate (HY-B1617A). Zuclomiphene citrate is a cis isomer of Clomiphene citrate (HY-B0463). Zuclomiphene citrate is orally active and has an antiestrogenic effect. Zuclomiphene can reduce cholesterol levels. Zuclomiphene citrate can be for the researches of endocrinology and metabolic disease.

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. . 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.

Estrogen receptor modulator 14 is a chromene-derived prodrug of selective Estrogen Receptor modulator with oral activity. Estrogen receptor modulator 14 undergoes hydrolysis in vivo to produce the active metabolite 2d-(R), which acts on ERα and ERβ. Estrogen receptor modulator 14 acts on central thermoregulatory sites and possesses the ability to regulate estrogen signaling in multiple systemic tissues. Estrogen receptor modulator 14 maintains antiestrogenic activity in the uterus, and alters plasma cholesterol and bone metabolism. Estrogen receptor modulator 14 can be used for the research of estrogen receptor-related diseases.

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.

NKS-01 is a selective estrogen receptor modulator. NKS-01 can be used for the research of cancer, such as estrogen receptor-positive breast cancer.

SR 16234 (TAS-108) is a selective estrogen receptor modulator. SR 16234 is promising for research of pain symptoms associated with endometriosis.

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.

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.

(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.

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.