Bazedoxifene hydrochloride (TSE-424 hydrochloride) 是一种有口服活性的，能透过血脑屏障的，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 hydrochloride 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 hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidalselectiveestrogen receptor modulator(SERM), withIC50s of 23 nM and 99 nM forERαandERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor ofIL-6/GP130protein-protein interactions. Bazedoxifene hydrochloride 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 hydrochloride is a small molecular GP130 inhibitor, which binds to GP130 D1 domain[1].
Bazedoxifene hydrochloride inhibits STAT3 phosphorylation induced by IL-6 and IL-11 in GP130/STAT3 pathway signaling[1].
Bazedoxifene hydrochloride (10 μM-20 μM; 2 hours) inhibits STAT3 phosphorylation induced by cytokines in human pancreatic cancer cells[2].
Bazedoxifene hydrochloride (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells[2].
Bazedoxifene hydrochloride inhibits STAT3 nuclear translocation induced by IL-6[2].
Bazedoxifene hydrochloride 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 hydrochloride (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 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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