Bazedoxifene acetate

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议

产品介绍

Bazedoxifene acetate (TSE-424 acetate) 是一种口服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。醋酸巴多昔芬可用于骨质疏松症的研究。 Bazedoxifene acetate 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。

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 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.
产品描述	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.