产品描述:
Ridaifen-B is an antagonist of estrogen receptor α (ERα; IC50 = 52.4 nM), an inverse agonist of cannabinoid (CB) receptor 2 (CB2; Ki = 43.7 nM), and a derivative of tamoxifen (Item No. 13258).{42930} It is selective for CB2 over CB1 receptors (Ki = 732 nM).{42931} Ridaifen-B was designed to be cytotoxic to cancer cells independent of ER binding; it inhibits growth of ER-positive and ER-negative cells in a panel of 39 cancer cell lines (GI50s = 0.20-2.14 µM).{42932} It induces apoptosis and autophagy in ER-negative Jurkat cells when used at a concentration of 0.4 µM.{42933} Ridaifen-B decreases nitric oxide (NO) production and protein levels of IL-1α and IL-6 in LPS-stimulated RAW 264.7 cells when used at a concentration of 1 µM.{42931}