Lasofoxifene (tartrate)
(Synonyms: 酒石酸拉索昔芬,CP 336,156) 目录号 : GC11425
A selective estrogen receptor modulator
Cas No.:190791-29-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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].
References:
[1]. Ke HZ, Paralkar VM, Grasser WA, 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. 1998 Apr;139(4):2068-76.
[2]. Cummings SR, Ensrud K, Delmas PD, et al. Lasofoxifene in postmenopausal women with osteoporosis. N Engl J Med. 2010 Feb 25;362(8):686-96.
[3]. Gennari L, Merlotti D, Nuti R. Selective estrogen receptor modulator (SERM) for the treatment of osteoporosis in postmenopausal women: focus on lasofoxifene. Clin Interv Aging. 2010 Feb 2;5:19-29.
[4]. Kumar P, Song ZH. CB2 cannabinoid receptor is a novel target for third-generation selective estrogen receptor modulators bazedoxifene and lasofoxifene. Biochem Biophys Res Commun. 2014 Jan 3;443(1):144-9.
| Cas No. | 190791-29-8 | SDF | |
| 别名 | 酒石酸拉索昔芬,CP 336,156 | ||
| 化学名 | (5R,6S)-5,6,7,8-tetrahydro-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2-naphthalenol, (2S,3S)-2,3-dihydroxybutanedioate | ||
| Canonical SMILES | OC(C=C1)=CC2=C1[C@@H](C3=CC=C(OCCN4CCCC4)C=C3)[C@@H](C5=CC=CC=C5)CC2.OC([C@@H](O)[C@H](O)C(O)=O)=O | ||
| 分子式 | C28H31NO2 • C4H6O6 | 分子量 | 563.6 |
| 溶解度 | ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7743 mL | 8.8715 mL | 17.7431 mL |
| 5 mM | 0.3549 mL | 1.7743 mL | 3.5486 mL |
| 10 mM | 0.1774 mL | 0.8872 mL | 1.7743 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。