Raloxifene 6,4'-Bis-β-D-glucuronide, a metabolite of Raloxifene, acts as a selective antagonist of the estrogen receptor used for osteoporosis prevention.
Methyl Raloxifene 4'-(2,3,4-Tri-O-acetyl-β-D-glycopyranuronate) is a derivative compound of Raloxifene 4'-glucuronide, designed to resemble its structure and function.
Compound 7, or Raloxifene 6-Monomethyl Ether, is a derivative of Raloxifene that effectively inhibits estrogen receptor α. It also displays the inhibitory effects on MCF-7 cells, with an IC50 of 250 nM and a pIC50 of 6.6.
Raloxifene 4-Monomethyl Ether (Compound 37) is a derivative of Raloxifene which acts as an inhibitor of estrogen receptor α. It effectively suppresses the activity of MCF-7 cells, exhibiting an IC50 value of 1 μM and a pIC50 value of 6.
4'-Raloxifene-β-D-glucopyranoside is a metabolite of Raloxifene. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist.
6-Raloxifene-β-D-glucopyranoside is a benzothiophene glucuronidated at the 6' position. It is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss, resorption, and lowering lipid
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator (SERM) exhibiting a fixed ring structure analogous to raloxifene. This compound demonstrates potent antiestrogenic effects on breast cancer and endometrium while displaying minimal side effects. Additionally, Arzoxifene elicits favorable estrogenic effects on bone health and lipid profile.
Silybin B (Silibinin B) 是雷洛昔芬4′-和6-葡萄糖醛酸化的有效抑制剂,是水飞蓟素有效的抗纤维原性和抗低聚物成分,具有清除1,1-二苯基-2-吡啶酰肼(DPPH)自由基的活性 ,可通过减轻 DNA 损伤和细胞凋亡对顺铂诱导的神经毒性具有保护作用。Silybin B 对人慢性髓系白血病 K562细胞的生长抑制和诱导凋亡有较强的作用。