醋酸巴多昔芬

作用机制用途生物活性靶点体外研究体内研究醋酸巴多昔芬试剂级价格

醋酸巴多昔芬

CAS号:198481-33-3
英文名:BAZEDOXIFENE ACETATE
中文名:醋酸巴多昔芬
CBNumber:CB71011079
分子式:C32H38N2O5
分子量:530.67
MOL File:198481-33-3.mol

醋酸巴多昔芬化学性质

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
SMILES :C(=O)(O)C.C(C1C=CC(OCCN2CCCCCC2)=CC=1)N1C2C=CC(O)=CC=2C(C)=C1C1C=CC(O)=CC=1

安全信息

WGK Germany :3

醋酸巴多昔芬性质、用途与生产工艺

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.

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.