Lasofoxifene (tartrate)

Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM)^[1]. Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis^[1][2]. IC50 & Target: Target: Estrogen Receptor^[1] In Vitro: Lasofoxifene tartrate (1 nM-1 μM; 48 h) shows antagonist activity on ER+ breast cancer cells without being affected by the expression level of activating ERα mutants relative to wild-type (WT) ERα^[2].
In Vivo: Lasofoxifene tartrate (4 mg/mice; s.c.; 5 day/week; for 43 d) decreases arthritis severity, by reducing cartilage oligomeric matrix protein (COMP), the serum marker of cartilage destruction and reducing serum IL-6 (inflammatory cytokine) levels^[1].
Lasofoxifene tartrate (4 mg/mice; s.c.; 5 day/week; for 43 d) protects against generalised bone loss in CIA by increasing trabecular bone mineral density (BMD), cortical thickness in mice^[1].
Lasofoxifene tartrate (5, and 10 mg/kg; s.c.; 5 day/week; for 70 d) exerts function of inhibiting primary tumor growth and reducing metastases to the lung and the liver in mice^[3].