Bazedoxifene acetate

A selective estrogen receptor modulator

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库存: 现货

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5mg

￥812.00

650.00

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10mg

￥1550.00

1240.00

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50mg

￥5337.00

4270.00

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货号: ajci5946
CAS: 198481-33-3
别名: 醋酸巴多昔芬,Viviant, WAY-140424, WAY-TES 424, Conbriza, TSE-424,
分子式: C32H38N2O5
分子量: 530.65
纯度: >98%
溶解度: ≥ 182 mg/mL in DMSO, ≥ 8.483 mg/mL in EtOH with ultrasonic and warming
储存: 4°C, protect from light
库存: 现货

Background

Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively.

参考文献:
[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.

Protocol

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.
参考文献: 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.