货号 | 10011620-50mg |
描述 | Selective estrogen receptor modulators (SERMs) are a class of pharmacologically active ER ligands that exert agonist and antagonist effects on various estrogen target tissues.1 They are designed to promote the beneficial actions of estrogen (e.g., bone maintenance and remodeling) while preventing its detrimental effects (e.g., growth of breast and endometrial cancers). Raloxifene, marketed under the name Evista®, is a selective estrogen receptor modulator (SERM) that exhibits estrogenic activity in bone cells without stimulating breast or uterine tissues.2 It has been approved for clinical use for prevention and treatment of postmenopausal osteoporosis. When administered at 60 mg/day for 12 weeks to postmenopausal, osteoporotic women, raloxifene reduced bone resportion, and promoted bone formation by decreasing serum levels of interleukin-6 and parathyroid hormone and increasing serum levels of 25-hydroxy vitamin D.3 Raloxifene reportedly guards endothelial cells obtained from rat aortic rings against oxidative insult (1 µM) and lowers serum cholesterol in ovariectomized rodents (ED50 = 0.2 mg/kg).4,2 |
别名 | Evista®;Keoxifene;LY156758; |
供应商 | Cayman |
应用文献 | |
1.Skouby, S.O. Criteria for the selection of an optimal estrogen replacement. Gynecological Endocrinology 15, 60-67 (2001). 2.Black, L.J.,Sato, M.,Rowley, E.R., et al. Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J. Clin. Invest. 93(1), 63-69 (1994). 3.Özmen, B.,Kirmaz, C.,Aydin, K., et al. Influence of the selective oestrogen receptor modulator (raloxifene hydrochloride) on IL-6, TNF-α, TGF-ß1 and bone turnover markers in the treatment of postmenopausal osteoporosis. Eur. Cyto. Netw. 18(3), 148-153 (2007). 4.Wong, C.M.,Yung, L.M.,Leung, F.P., et al. Raloxifene protects endothelial cell function against oxidative stress. Br. J. Pharmac. 155(3), 326-334 (2008). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 510.2 |
分子式 | C28H27NO4S • HCl |
CAS号 | 82640-04-8 |
稳定性 | ≥ 2 years |
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