GlpBio

Bazedoxifene acetate

目录号: GC10852纯度: >99.50%同义词: 醋酸巴多昔芬,Viviant, WAY-140424, WAY-TES 424, Conbriza, TSE-424,
A selective estrogen receptor modulator
Bazedoxifene acetate
Cas No.: 198481-33-3
规格价格库存数量操作
5mg¥1,125.00现货
1
10mg¥1,665.00现货
1
25mg¥2,664.00现货
1
50mg¥3,726.00现货
1
100mg¥4,860.00现货
1
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产品描述 Description

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.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

MCF-7 human mammary carcinoma cells

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.

Reacting condition

10−8 to 10−6 M Bazedoxifene acetate for 24 hours.

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]:

Animal models

Sprague Dawley rats

Dosage form

0.1, 0.3, 1.0, and 3.0 mg/kg per day for 6 weeks

Preparation method

Bazedoxifene was administered orally in a saline, Tween-80, methylcellulose vehicle.

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.

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.

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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
198481-33-3
同义词
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
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 g/mol
溶解性
≥ 182 mg/mL in DMSO, ≥ 8.483 mg/mL in EtOH with ultrasonic and warming
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol