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Bazedoxifene hydrochloride (Synonyms: TSE-424 hydrochloride)

目录号: HY-A0031A
产品使用指南

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。

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Bazedoxifene hydrochloride Chemical Structure

Bazedoxifene hydrochloride Chemical Structure

CAS No. : 198480-56-7

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Description

Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].

IC50 & Target

IC50: 26 nM (ERα), 99 nM (ERβ)[1]

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.
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.
Molecular Weight

507.06

Formula

C₃₀H₃₅ClN₂O₃

CAS No.

198480-56-7

中文名称

盐酸巴多昔芬

SMILES

OC1=CC2=C(N(CC3=CC=C(OCCN4CCCCCC4)C=C3)C(C5=CC=C(O)C=C5)=C2C)C=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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× = ×
C1   V1   C2   V2

Keywords:

BazedoxifeneTSE-424TSE424TSE 424Estrogen Receptor/ERRselectiveestrogenreceptormodulatorSERMERαERβIL-6/GP130protein-proteininteractionsSTAT3Inhibitorinhibitorinhibit

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产品名称:
Bazedoxifene hydrochloride
目录号:
HY-A0031A
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