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化學性質:
規格 | 10mg 25mg 50mg |
CAS | 190791-29-8 |
別名 | CP 336,156 |
化學名 | (5R,6S)-5,6,7,8-tetrahydro-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2-naphthalenol, (2S,3S)-2,3-dihydroxybutanedioate |
分子式 | C28H31NO2 • C4H6O6 |
分子量 | 563.6 |
溶解度 | ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
Lasofoxifene (tartrate) is a third-generation, nonsteroidal selective estrogen receptor modulator (SERM).
Estrogen receptors are activated by the hormone estrogen (17β-estradiol). SERMs are characterized by having estrogen agonist action in some tissues while acting as estrogen antagonists in others [1][2].
Lasofoxifene, also known as CP 336,156, is a third-generation, nonsteroidal selective estrogen receptor modulator. Lasofoxifene bound with high affinity to the human estrogen receptor-α with IC50 value of 1.5 nM [1]. Lasofoxifene is also a CB2 inverse agonist [4].
In aged female rats, Lasofoxifene decreased total serum cholesterol and fat body mass, and no uterine hypertrophy was observed. In 5-month-old ovariectomized (OVX) Sprague-Dawley female rats, Lasofoxifene completely prevented OVX-induced increases in body weight gain, total serum cholesterol, and serum osteocalcin. CP-336,156 completely prevented OVX-induced bone loss and inhibited the increased bone turnover associated with estrogen deficiency in lumbar vertebrae, proximal tibiae, and distal femora [1].
In postmenopausal women with osteoporosis, lasofoxifene 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].
特別提醒:
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278