estrogen receptor modulator

Enclomiphene citrate (trans-Clomiphene citrate) is a non-steroidal estrogen receptor antagonist,with antioestrogenic property

Estrogen receptor modulator 1 causes regression of Tamoxifen-resistant, hormone-independent xenograft tumors. Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM) (pIC50: 0.46).

Estrogen receptor modulator 6 (compound 3a) is a highly specific and potent agonist of the estrogen receptor (ER) β, exhibiting remarkable affinity (K i = 0.44 nM) and impressive 19-fold selectivity for ERβ over ERα, as evidenced by its affinity (K i = 8.4 nM).

Estrogen Receptor Modulator 7 is a potent modulator of estrogen receptors, utilized in cancer research [1].

Estrogen Receptor Modulator 8 (compound 4) is an orally active inhibitor targeting Estrogen Receptor ERR α with potent efficacy (IC50 = 0.437 nM in MCF-7 cells) and effectively hampers MCF-7 cell proliferation (IC50 = 0.1 nM) [1].

Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1 G0 phase, making it applicable in cancer research [1].

Estrogen receptor modulator11 (Compound 27) is a tetrahydroisoquinoline derivative. It exhibits affinity for the estrogen receptor (ER), with IC50 values of 285 nM for ERα and 421 nM for ERβ. Estrogen receptor modulator11 does not demonstrate antagonist activity in MCF-7 cell assays.

Estrogen receptor modulator13 (Compound 5D) is an estrogen receptor antagonist with significant cytotoxic effects on MCF7 cells, exhibiting an IC50 value of 8.50 μM. Estrogen receptor modulator13 holds potential for breast cancer research.

4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

Pipendoxifene hydrochloride is a selective modulator of estrogen receptor.

Fispemifene (HM-101) is an estrogen receptor modulator (SERM) used to treat genitourinary syndromes and vaginal atrophy.

CHF-4227 is a novel, potent and selective estrogen receptor modulator that reduces cholesterol and LDL cholesterol concentrations.

Tamoxifen Citrate is an orally active selective estrogen receptor modulator (SERM) that blocks estrogen activity in breast cells while activating estrogen signaling in cells such as those of the bone, liver, and uterus. As an Hsp90 activator, it enhances the ATPase activity of the Hsp90 chaperone complex, induces autophagy and apoptosis, and can be used to generate gene knockout models in CreER(T2) transgenic mice as well as liver injury models.

Clomiphene citrate (NSC 35770) is a selective estrogen receptor modulator.

Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Bazedoxifene acetate (WAY-TES 424) is a novel selective estrogen receptor modulator (SERM).

Chlorotrianisene (tri-p-anisylchloroethylene) is an orally bioavailable, highly lipophilic, synthetic triphenylethylene (TPE) derivative and selective estrogen receptor modulator (SERM), with predominantly estrogenic but also antiestrogenic activities.

Bazedoxifene hydrochloride (TSE 424 hydrochloride) is an orally active, selective, and potent estrogen receptor modulator (SERM) that crosses the blood-brain barrier and is an inhibitor of IL-6 GP130 protein interactions with high affinity for ERα and ERβ. It has a high affinity for ERα and ERβ and can be used to study postmenopausal osteoporosis and vasodilator-related diseases.

Toremifene (GTx 006) is a selective estrogen-receptor modulator (SERM).

Arzoxifene hydrochloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue.

Ospemifene D4 is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active modulator of estrogen receptor.

Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen is a selective modulator of estrogen receptor (SERM). Tamoxifen is a potent activator of Hsp90 and enhances the Hsp90 molecular chaperone ATPase activity.

Idoxifene is a tissue-specific selective estrogen receptor modulator.