Lasofoxifene Tartrate 是一种非甾体类的雌激素受体选择性调节剂 (SERM)。
产品描述
Lasofoxifene Tartrate is a third-generation, non-steroidal selective estrogen receptor modulator.
体内活性
Lasofoxifene (LAS) and BZA reduced the clinical severity of arthritis as well as the grade of histologic synovitis and erosions on cartilage and bone.?Moreover, SERMs protected against generalised bone loss in CIA by increasing trabecular BMD.?Both SERMs decreased serum marker of cartilage destruction and LAS reduced serum IL-6 levels.?SERMs did not alter Th17 cells in lymph nodes as E2 did[1].
动物实验
Female DBA/1 mice were ovariectomised and subjected to CIA as a model of post-menopausal RA. Mice received treatment with Lasofoxifene (LAS), BZA, 17β-estradiol (E2) as reference or vehicle. Arthritis development was assessed and BMD was determined by peripheral quantitative CT of the femurs. Serologic markers of inflammation and cartilage destruction were analysed. Immune cells in lymph nodes were studied by flow cytometry[1].
Cas No.
190791-29-8
分子式
C32H37NO8
分子量
563.647
别名
酒石酸拉索昔芬;CP-336156
储存和溶解度
DMSO:6 mg/mL (10.65 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years