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。
| 生物活性 | Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidalselectiveestrogen receptor modulator(SERM), withIC50s of 23 nM and 99 nM forERαandERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor ofIL-6/GP130protein-protein interactions and can be used for the research of pancreaticcancer[1][2]. |
| IC50& Target | IC50: 26 nM (ERα), 99 nM (ERβ)[1] |
体外研究
(In Vitro) | Bazedoxifene acetate is a small molecular GP130 inhibitor, which binds to GP130 D1 domain[1].
Bazedoxifene acetate inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling[1].
Bazedoxifene acetate (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells[2].
Bazedoxifene acetate (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells[2].
Bazedoxifene acetate inhibits STAT3 nuclear translocation induced by IL-6[2].
Bazedoxifene acetate blocks the cells migration in pancreatic cancer cells by inhibition of GP130[2].
Western Blot Analysis[2] | 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[2] | 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. |
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体内研究
(In Vivo) | Bazedoxifene acetate (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo[2].
| Animal Model: | 6-week-old female athymic nude mice[2] | | Dosage: | 5 mg/kg | | Administration: | Oral gavage, daily, for 18 days | | Result: | Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(188.45 mM) H2O : 1 mg/mL(1.88 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.8845 mL | 9.4224 mL | 18.8448 mL | | 5 mM | 0.3769 mL | 1.8845 mL | 3.7690 mL | | 10 mM | 0.1884 mL | 0.9422 mL | 1.8845 mL |
*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。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 5% DMSO 40%PEG300 5%Tween-80 50% saline Solubility: ≥ 2.75 mg/mL (5.18 mM); Clear solution 2. 请依序添加每种溶剂： 5% DMSO 95% (20%SBE-β-CDin saline) Solubility: ≥ 2.75 mg/mL (5.18 mM); Clear solution 3. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.71 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 4. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.71 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 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: ≥ 2.5 mg/mL (4.71 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.71 mM，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 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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