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Bazedoxifene acetate
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。
Bazedoxifene acetate图片
CAS NO:198481-33-3
包装:10mg, 50mg
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品名称
TSE 424
WAY-TES 424
产品介绍

生物活性

Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Pfizer are seeking approval for bazedoxifene in the prevention and treatment of postmenopausal osteoporosis. Bazedoxifene’s combination with conjugated estrogens, Aprela, is currently undergoing Phase III studies.


化学数据

分子量530.65
分子式C30H34N2O3.C2H4O2
CAS号198481-33-3
纯度>98%
溶解性(25°C)DMSO
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系MCF-7
方法For the proliferation assay, plating cells at 20,000 cells/well in a 24-well plate in DMEM/F12 (50:50) (phenol red-free) with 10% charcoal/dextran-treated FBS and 1 × GlutaMAX-1.Overnight incubation later, the medium is aspirated and treatments in DMEM/F12 (50:50) (phenol red-free) with 2% charcoal/dextran-treated FBS and 1 × GlutaMAX-1 are added to the wells. Each plate has a vehicle (baseline proliferation) and treatments. Treatments included 10 pM 17β-estradiol determined to be the EC80 for 17β-estradiol and 17β-estradiol in combination with six concentrations of BZA. Treatments from d 1 are renewed on d 3 and d 6 by aspirating medium from wells and replacing with fresh medium and treatments. On d 7, using trypsin-EDTA and counted using a Multisizer II to detach cell from the plate .
浓度~10 nM
处理时间7 days

动物实验
动物模型Sprague Dawley rats
配制50% dimethylsulfoxide-50% 1× Dulbecco’s PBS
剂量0.5 and 5.0 mg/kg
给药处理SC

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM1.8845 mL9.4224 mL18.8448 mL
5 mM0.3769 mL1.8845 mL3.769 mL
10 mM0.1884 mL0.9422 mL1.8845 mL