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 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 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 / Mass | 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 |
