醋酸巴多昔芬
| 中文名称 | 醋酸巴多昔芬 |
|---|---|
| 中文同义词 | 醋酸巴多西芬;巴多昔芬醋酸盐;醋酸巴泽昔芬;醋酸巴多昔芬;醋酸巴多昔芬 标准品;巴多昔芬乙酸酯;醋酸巴泽多西芬;1-(4-(2-(氮杂环庚烷-1-基)乙氧基)苄基)-2-(4-羟基苯基)-3-甲基-1H-吲哚-5-醇 乙酸盐 |
| 英文名称 | BAZEDOXIFENE ACETATE |
| 英文同义词 | BAZEDOXIFENE ACETATE;1-(p-(2-(Hexahydro-1H-azepin-1-yl)ethoxy)benzyl)-2-(p-hydroxyphenyl)-3-methylindol-5-ol monoacetate (salt);1H-Indol-5-ol, 1-((4-(2-(hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-, monoacetate (salt);Bazedoxifene acetate [usan];Unii-J70472ud3d;Viviant;Way-140424;1-((4-(2-(Hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol monoacetate |
| CAS号 | 198481-33-3 |
| 分子式 | C32H38N2O5 |
| 分子量 | 530.67 |
| EINECS号 | 638-804-4 |
| 相关类别 | 原料药;医药中间体;小分子抑制剂，天然产物;小分子抑制剂;醋酸巴多昔芬;医用原料;医药原料;Bazedoxifene Acetate;Inhibitors;API原料药-兽药原料药;日用化学品;试剂盒-细胞分析试剂盒;活性小分子库;化学试剂 |
| Mol文件 | 198481-33-3.mol |
| 结构式 |  |
醋酸巴多昔芬 性质
| 熔点 | 174-178° |
|---|---|
| 储存条件 | -20°C |
| 溶解度 | DMSO：可溶15mg/mL，澄清 |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| InChIKey | DGEPGJZKMFNSDD-UHFFFAOYSA-N |
| SMILES | C(=O)(O)C.C(C1C=CC(OCCN2CCCCCC2)=CC=1)N1C2C=CC(O)=CC=2C(C)=C1C1C=CC(O)=CC=1 |
醋酸巴多昔芬的作用机制具有独特之处，是一种新型的选择性雌激素受体调节剂(SERM)，对雌激素受体具有选择性的调节作用。巴多昔芬在身体的某些组织具有雌激素受体激动作用，在人体骨骼具有和雌激素相同的作用(雌激素可延缓骨老化，降低骨折发生)。
醋酸巴昔芬是一种非甾体选择性雌激素受体调节剂(SERM)。醋酸巴昔芬用于抗骨质疏松。Bazedoxifene acetate (TSE-424 acetate) 是一种有口服活性的，非甾体、选择性的雌激素受体调节剂 (SERM)，对 ERα 和 ERβ 作用的 IC50 值分别为 26 nM 和 99 nM，可用于骨质疏松症的研究。Bazedoxifene acetate 也是一种 IL-6/GP130 蛋白相互作用抑制剂，可用于胰腺癌的研究。IC50: 26 nM (ERα), 99 nM (ERβ)
Bazedoxifene acetate is a small molecular GP130 inhibitor, which binds to GP130 D1 domain.
Bazedoxifene acetate inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling.
Bazedoxifene acetate (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells.
Bazedoxifene acetate (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells.
Bazedoxifene acetate inhibits STAT3 nuclear translocation induced by IL-6.
Bazedoxifene acetate blocks the cells migration in pancreatic cancer cells by inhibition of GP130.
Western Blot Analysis
| Cell Line: | AsPC-1 cells |
| Concentration: | 10 μM, 20 μM |
| Incubation Time: | 2 hours |
| Result: | Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation. |
Apoptosis Analysis
| Cell Line: | Capan-1 cells, BxPC-3 cells, HPAF-II cells, HPAC cells |
| Concentration: | 10 μM, 20 μM (Capan-1); 5 μM, 10 μM (BxPC-3); 10 μM, 20 μM (HPAF-II); 10 μM, 15 μM (HPAC) |
| Incubation Time: | Overnight |
| Result: | Induced apoptosis. |
Bazedoxifene acetate (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo.
| Animal Model: | 6-week-old female athymic nude mice |
| Dosage: | 5 mg/kg |
| Administration: | Oral gavage, daily, for 18 days |
| Result: | Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells. |
安全信息
| WGK Germany | 3 |
|---|
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-A0036 | 醋酸巴多昔芬 Bazedoxifene acetate | 198481-33-3 | 5mg | 500元 |
| 2024/04/30 | HY-A0036 | 醋酸巴多昔芬 Bazedoxifene acetate | 198481-33-3 | 10mM * 1mLin DMSO | 580元 |