| 货号 | 17646-5mg |
| 描述 | Lasofoxifene is a third-generation, non-steroidal selective estrogen receptor modulator (SERM). It selectively binds to human ERα with an IC50 value of 1.5 nM and inhibits bone loss in ovariectomized rats.1 In clinical studies of postmenopausal osteoporosis, 0.5 mg/day lasofoxifene was associated with reduced risks of nonvertebral and vertebral fractures, ER-positive breast cancer, coronary heart disease, and stroke but an increased risk of venous thromboembolic events.2,3 Lasofoxifene has also been shown to act as an inverse agonist at the CB2 cannabinoid receptor, indicating its potential to be repurposed as a therapeutic for indications wherein CB2 is a target.4 |
| 别名 | CP 336,156; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ke, H.Z.,Paralkar, V.M.,Grasser, W.A., et al. Effects of CP-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus, and body composition in rat models. Endocrinology 139(4), 2068-2076 (1998). 2.Cummings, S.R.,Ensrud, K.,Delmas, P.D., et al. Lasofoxifene in postmenopausal women with osteoporosis. New England Journal of Medicine 362(8), 686-696 (2010). 3.Gennari, L.,Merlotti, D. and Nuti, R. Selective estrogen receptor modulator (SERM) for the treatment of osteoporosis in postmenopausal women: Focus on lasofoxifene. Clinical Interventions in Aging 5, 19-29 (2010). 4.Kumar, P. and Song, Z.H. CB2 cannabinoid receptor is a novel target for third-generation selective estrogen receptor modulators bazedoxifene and lasofoxifene. Biochem.Bioph.Res.Co. 443, 144-149 (2014). | |
| 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 | 563.6 |
| 分子式 | C28H31NO2 • C4H6O6 |
| CAS号 | 190791-29-8 |
| 稳定性 | ≥ 2 years |
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