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
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:
C30H34N2O3.C2H4O2
分子量:
530.661
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
Mol文件:
198481-33-3.mol
熔点
174-178°
储存条件
?20°C
溶解度
DMSO: soluble15mg/mL, clear
形态
powder
颜色
white to beige
InChIKey
DGEPGJZKMFNSDD-UHFFFAOYSA-N
作用机制
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)。
用途
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。
生物活性
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。
靶点
IC50: 26 nM (ERα), 99 nM (ERβ)
体外研究
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.
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.
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.
体内研究
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.
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.
WGK Germany
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