Bazedoxifene acetate
(Synonyms: 醋酸巴多昔芬,Viviant, WAY-140424, WAY-TES 424, Conbriza, TSE-424,) 目录号 : GC10852
A selective estrogen receptor modulator
Cas No.:198481-33-3
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
| Cell experiment [1]: | |
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Cell lines |
MCF-7 human mammary carcinoma cells |
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Preparation method |
Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10−8 to 10−6 M Bazedoxifene acetate for 24 hours. |
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Applications |
Bazedoxifene acetate down-regulates ERα protein in MCF-7:5C and MCF-7:2A Cells. It also inhibits ERα transcriptional activity, blocks cell cycle progression in MCF-7:5C cells and down-regulates cyclin D1. |
| Animal experiment [2]: | |
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Animal models |
Sprague Dawley rats |
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Dosage form |
0.1, 0.3, 1.0, and 3.0 mg/kg per day for 6 weeks |
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Preparation method |
Bazedoxifene was administered orally in a saline, Tween-80, methylcellulose vehicle. |
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Application |
Dose response data for Bazedoxifene acetate demonstrate consistent, significant increased bone mass, compared with control animals via pQCT evaluation is achieved at 0.1 mg/kg per day with increases at 0.3, 1.0, and 3.0 mg/kg per day. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Lewis-Wambi JS, Kim H, Curpan R, Grigg R, Sarker MA, Jordan VC. The selective estrogen receptor modulator bazedoxifene inhibits hormone-independent breast cancer cell growth and down-regulates estrogen receptor α and cyclin D1. Mol Pharmacol. 2011 Oct;80(4):610-20. 2. Komm BS, Kharode YP, Bodine PV, Harris HA, Miller CP, Lyttle CR. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity.Endocrinology. 2005 Sep;146(9):3999-4008. | |
Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively.
References:
[1]. Jaime Kulak, et al. Treatment with Bazedoxifene, a Selective Estrogen Receptor Modulator, Causes Regression of Endometriosis in a Mouse Model. Endocrinology. 2011; 152(8): 3226-3232.
[2]. Hisaya Kawate, Ryoichi Takayanagi. Efficacy and safety of bazedoxifene for postmenopausal osteoporosis. Clin Interv Aging. 2011; 6: 151-160.
[3]. Stefano Lello, et al. Bazedoxifene: literature data and clinical evidence. Clin Cases Miner Bone Metab. 2011; 8(3): 29-32.
[4]. Joan S. Lewis-Wambi, Helen Kim, Ramona Curpan, et al. The Selective Estrogen Receptor Modulator Bazedoxifene Inhibits Hormone-Independent Breast Cancer Cell Growth and Down-Regulates Estrogen Receptor α and Cyclin D1. Mol Pharmacol. 2011 ; 80(4): 610-620.
[5]. Diane M Biskobing. Update on bazedoxifene: A novel selective estrogen receptor modulator. Clin Interv Aging. 2007; 2(3): 299-303.
| Cas No. | 198481-33-3 | SDF | |
| 别名 | 醋酸巴多昔芬,Viviant, WAY-140424, WAY-TES 424, Conbriza, TSE-424, | ||
| 化学名 | acetic acid;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.CC(=O)O | ||
| 分子式 | C32H38N2O5 | 分子量 | 530.65 |
| 溶解度 | ≥ 182 mg/mL in DMSO, ≥ 8.483 mg/mL in EtOH with ultrasonic and warming | 储存条件 | 4°C, protect from light |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8845 mL | 9.4224 mL | 18.8448 mL |
| 5 mM | 0.3769 mL | 1.8845 mL | 3.769 mL |
| 10 mM | 0.1884 mL | 0.9422 mL | 1.8845 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。