Raloxifene hydrochloride

Raloxifene, also known as LY-139481, is a selective benzothiophene estrogen receptor modulator (SERM). Raloxifene binds to estrogen receptors (ER) as a mixed estrogen agonist/antagonist; it displays both an ER-alpha-selective partial agonist/antagonist effect and a pure ER-beta-selective antagonist effect. This agent functions as an estrogen agonist in some tissues (bones, lipid metabolism) and as an estrogen antagonist in others (endometrium and breasts), with the potential for producing some of estrogen's beneficial effects without producing its adverse effects.

Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.

Estrogen/progestogen Receptor Inhibitors Related Products:

Fulvestrant; Lasofoxifene Tartrate; Brilanestrant; Tamoxifen; Tamoxifen citrate; Dienogest; Drospirenone; Ulipristal acetate; Megestrol Acetate; Pregnenolone; Estriol; Estrone; Bazedoxifene Acetate; Endoxifen HCl; Ospemifene; AZD9496; Desogestrel

[1]. Yang, N.N., et al., Estrogen and raloxifene stimulate transforming growth factor-beta 3 gene expression in rat bone: a potential mechanism for estrogen- or raloxifene-mediated bone maintenance. Endocrinology, 1996. 137(5): p. 2075-84.

[2]. Obach, R.S., Potent inhibition of human liver aldehyde oxidase by raloxifene. Drug Metab Dispos, 2004. 32(1): p. 89-97.

[3]. Sato, M., M.K. Rippy, and H.U. Bryant, Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats. FASEB J, 1996. 10(8): p. 905-12.