Bazedoxifene
(Synonyms: 巴多昔芬; TSE-424) 目录号 : GC14883
Bazedoxifene (TSE-424) 是一种口服的、可渗透 BBB 的非甾体选择性雌激素受体调节剂 (SERM)，对 ERα 和 ERβ 的 IC50 分别为 23 nM 和 99 nM。巴多昔芬可用于骨质疏松症的研究。 Bazedoxifene 还作为 IL-6/GP130 蛋白-蛋白相互作用的抑制剂，可用于胰腺癌的研究。
Cas No.:198481-32-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Bazedoxifene is a selective estrogen receptor modulator (SERM) with IC50 value of 26 and 99 nM for estrogen receptorα and β, respectively [1].
Bazedoxifene is a SERM used for the prevention and treatment of post menopausalo steoporosis which is caused by the loss of endogenous levels of estrogens. It is developed as a third-generation SERM which can reduce the vertebral and nonvertebral fracture risk and have no stimulatory effects on breast or uterus. Bazedoxifene is an estrogen receptor ligand with an indole-based core binding domain. It binds to both ERα (IC50 value of 23nM) and ERβ (IC50 value of 85nM), exhibited agonist activity in bone, cardiovascular system and CNS while exhibited antagonist activity in breast and endometrium. It competitively inhibited the binding of 17β-estradiol to both ERα and ERβ [1, 2 and 3].
In MCF7 cells, treatment of bazedoxifene showed no ER agonist activity and no effect on the cell proliferation. However, it suppressed the 17β-estradiol -induced transcriptional activation and cell proliferation [3].
In ovariectomized rats, administration of bazedoxifene at dose of 0.3 or 3.0 mg /kg daily for 6 weeks resulted in the protection of skeleton from bone loss with increased bone mineraldensity. In addition, the compression strength of the fifth lumbar vertebra was significantly improved by bazedoxifene. Moreover, administration of bazedoxifene at dose of3.0 mg /kg/day showed modest stimulatory effects on rat uterine with small increase in wet uterine weight. Bazedoxifene also had no ER agonist effects on rat vasomotor activity [2 and 3].
References:
[1] de Villiers TJ. Bazedoxifene: a novel selective estrogen receptor modulator for postmenopausal osteoporosis. Climacteric. 2010 Jun;13(3):210-8.
[2] Duggan ST, McKeage K. Bazedoxifene: a review of its use in the treatment of postmenopausal osteoporosis. Drugs. 2011 Nov 12;71(16):2193-212.
[3] Kawate H, Takayanagi R. Efficacy and safety of bazedoxifene for postmenopausal osteoporosis. Clin Interv Aging. 2011;6:151-60.
| Cas No. | 198481-32-2 | SDF | |
| 别名 | 巴多昔芬; TSE-424 | ||
| 化学名 | 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol | ||
| Canonical SMILES | CC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O | ||
| 分子式 | C30H34N2O3 | 分子量 | 470.6 |
| 溶解度 | Soluble in DMSO | 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 | 2.1249 mL | 10.6247 mL | 21.2495 mL |
| 5 mM | 0.425 mL | 2.1249 mL | 4.2499 mL |
| 10 mM | 0.2125 mL | 1.0625 mL | 2.1249 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。