antiestrogen

EM-651 (2H-1-Benzopyran-7-ol, 3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-, (2R)-) is an enantiomer of EM-652, IC50=20.0 nM. EM-652 is an orally active pure antiestrogen and selective estrogen receptor antagonist, IC50=0.44nM.

N-Desmethyltamoxifen hydrochloride is the primary metabolite of tamoxifen in humans.

Bexirestrant is an orally active ER-α degrader commonly employed in antiestrogen and antineoplastic therapy research.

Anordiol is an antiestrogen with estrogenic activity. It also is known to inhibit fertility.

PBPE hydrochloride is a derivative of tamoxifen and functions as a selective ligand for antiestrogen binding sites (AEBS). The binding affinity (Ki) of PBPE hydrochloride and MBPE to AEBS is 8.79 nM and 17.57 nM, respectively.

Clometherone is a synthetic pregnane steroid and derivative of progesterone which is used as an antiestrogen and antiandrogen.

GW7604 is an antiestrogen and it also is the metabolite of GW5638. GW5638 is an antagonist of high-affinity estrogen receptor (ER).

Trioxifene mesylate is an antiestrogen that suppresses growth hormone secretion.

Pure antiestrogen that downregulates estrogen receptor expression

OP-1074 is a pure antiestrogen and a selective degrader of ER, demonstrating specific antiestrogenic activity for ERα and ERβ.

Pachyaximine A possesses significant antibacterial activity against Escherichia coli, Staphylococcus aureus, Corynebacterium diphtheriae and Corynebacterium pyrogenes. (-)-Pachyaximine A demonstrates significant activity as antiestrogen binding site (AEBS

Axillaridine A is a new cholinesterase inhibitors, it may act as potential leads in the discovery of clinically useful inhibitors for nervous-system disorders, particularly by reducing memory deficiency in Alzheimer's disease patients by potentiating and

Pipendoxifene, also known as ERA-923, is a new antiestrogen with potential anticancer activity. ERA-923 potently inhibits estrogen binding to ER-alpha (IC50 = 14 nM). In ER-alpha-positive human MCF-7 breast carcinoma cells, ERA-923 inhibits estrogen-stimulated growth (IC50 = 0.2 nM) associated with cytostasis. In vitro, a MCF-7 variant with inherent resistance to tamoxifen (10-fold) or 4-OH tamoxifen (>1000-fold) retains complete sensitivity to ERA-923 . In preclinical models, ERA-923 has an improved efficacy and safety compared with tamoxifen. In the combination with temsirolimus, ERA-923 showed excellent anticancer activity in preclinical models.