中文名称: | 醋酸巴多昔芬 | ||||
---|---|---|---|---|---|
英文名称: | Bazedoxifene acetate | ||||
别名: | 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 TSE-424 acetate | ||||
CAS No: | 198481-33-3 | 分子式: | C32H38N2O5 | 分子量: | 530.665 |
CAS No: | 198481-33-3 | ||||
分子式: | C32H38N2O5 | ||||
分子量: | 530.665 |
基本信息
产品编号: |
B11543 |
||||
产品名称: |
Bazedoxifene acetate |
||||
CAS: |
198481-33-3 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
||||
分子式: |
溶于液体 |
-80℃ |
两年 |
||
分子量 |
530.66 |
-20℃ |
一个月 |
||
化学名: |
1-(4-(2-(azepan-1-yl)ethoxy)benzyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetate |
||||
Solubility (25°C): |
|||||
体外:
|
DMSO |
100mg/mL (188.44mM) |
|||
Ethanol |
25mg/mL warmed with 50ºC water bath (47.11mM) |
||||
Water |
Insoluble |
||||
体内(现配现用): |
1.请依序添加每种溶剂:5% DMSO→40% PEG300→5% Tween-80→50% saline Solubility: ≥ 2.75mg/mL (5.18mM); Clear solution 2.请依序添加每种溶剂:5% DMSO→95% (20% SBE-β-CD in saline) Solubility: ≥ 2.75mg/mL (5.18mM); Clear solution 3.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.5mg/mL (4.71mM); Clear solution |
||||
此⽅案可获得 ≥ 2.5mg/mL (4.71mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中,混合均匀;向上述体系中加⼊ 50μL Tween-80,混合均匀;然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 |
|||||
4.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5mg/mL (4.71mM); Clear solution |
|||||
此⽅案可获得 ≥ 2.5mg/mL (4.71mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混合均匀。 |
|||||
5.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility: ≥ 2.5mg/mL (4.71mM); Clear solution |
|||||
此⽅案可获得 ≥ 2.5mg/mL (4.71mM,饱和度未知) 的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例,取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中,混合均匀。 |
|||||
<1mg/ml表示微溶或不溶。 |
|||||
普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
|||||
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.8845mL |
9.4224mL |
18.8448mL |
5mM |
0.3769mL |
1.8845mL |
3.7690mL |
10mM |
0.1884mL |
0.9422mL |
1.8845mL |
50mM |
0.0377mL |
0.1884mL |
0.3769mL |
生物活性
产品描述 |
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 26nM 和 99nM,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 |
estrogen receptor |
|
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 (10μM-20μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells[2] . Bazedoxifene acetate (5-20μM; 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: |
10μM, 20μM |
|
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: |
10μM, 20μM (Capan-1); 5μM, 10μM (BxPC-3); 10μM, 20μM (HPAF-II); 10μM, 15μM (HPAC) |
|
Incubation Time: |
Overnight |
|
Result: |
Induced apoptosis. |
|
体内研究 |
Bazedoxifene acetate (5mg/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: |
5mg/kg |
|
Administration: |
Oral gavage, daily, for 18 days |
|
Result: |
Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )