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Bazedoxifene hydrochloride

产品编号 T6404 CAS 198480-56-7

别名: Bazedoxifene HCl, 盐酸巴多昔芬, TSE-424

Bazedoxifene hydrochloride (TSE-424) 是一种 IL-6/GP130蛋白相互作用抑制剂，可用于胰腺癌的研究。它也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，可用于研究骨质疏松症。

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Bazedoxifene hydrochloride Chemical Structure

Bazedoxifene hydrochloride, CAS 198480-56-7

规格	价格/CNY	货期
2 mg	￥ 713	待询
5 mg	￥ 1,279	待询
10 mg	￥ 2,304	待询
25 mg	￥ 3,591	待询
50 mg	￥ 6,461	待询
1 mL * 10 mM (in DMSO)	￥ 2,304	待询

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Bazedoxifene hydrochloride 的其他形式现货产品:

Bazedoxifene acetate

其他形式的 Bazedoxifene hydrochloride:

Bazedoxifene acetate
现货

DATASHEET SDS

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Bazedoxifene hydrochloride (TSE-424) is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively.
靶点活性	ERβ:89 nM, ERα:23 nM
体外活性	Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Bazedoxifene does not stimulate ERα mediated transcriptional activity and acts as an antagonist to estradiol in cultured breast cancer (bMCF-7) cells. Similar results are seen in other cell lines including CHO (ovarian), HepG2 (hepatic) or GTI-7 (neuronal) with bazedoxifene having no ERα agonist activity and acting as an antagonist to estradiol action.[2] Bazedoxifene does not stimulate proliferation of MCF-7 cells but did inhibit 17β-estradiol-induced proliferation with IC50 of 0.19 nM. [3]
体内活性	In an immature rat model, bazedoxifene increases uterine wet weight 35% at a dose of 0.5 mg/kg compared to an 85% increase with raloxifene at the same dose and a 300% increase in uterine weight with ethinyl estradiol at a dose of 10 μg/kg. Ovarectomized rats treated with 0.3 mg/d bazedoxifene displayed maintenance of bone mass and bone strength similar to effects seen with 2 μg/d ethinyl estradiol, 3 mg/d raloxifene, or sham operated animals. [2]
激酶实验	Ligand binding competition experiments: Test compounds are initially solubilized in DMSO and the final concentration of DMSO in the binding assay is ≤ 1%. Eight dilutions of each test compound are used as an unlabelled competitor for [3H]17β-estradiol. Typically, a set of compound dilutions would be tested simultaneously on human, rat and mouse ER-α and ER-β. The results are plotted as measured DPM vs. concentration of test compound. For dose-response curve fitting, a four parameter logistic model on the transformed, weighted data are fit and the IC50 is defined as the concentration of compound decreasing maximum [3H]estradiol binding by 50%. For active compounds, the IC50 is determined at least three times. It should be noted that IC50 values are not direct measures of a ligand's affinity for the receptor. Rather, they can only be compared as relative values, in this case to 17β-estradiol.
细胞实验	For the proliferation assay, cells are plated at 20,000 cells/well in a 24-well plate in DMEM/F12 (50:50) (phenol red-free) with 10% charcoal/dextran-treated FBS and 1 × GlutaMAX-1. After overnight incubation, the medium is aspirated and treatments in DMEM/F12 (50:50) (phenol red-free) with 2% charcoal/dextran-treated FBS and 1 × GlutaMAX-1 are added to the wells. Each plate has a vehicle (baseline proliferation) and treatments. Treatments included 10 pM 17β-estradiol determined to be the EC80 for 17β-estradiol and 17β-estradiol in combination with six concentrations of BZA. Treatments from d 1 are renewed on d 3 and d 6 by aspirating medium from wells and replacing with fresh medium and treatments. On d 7, cells are detached from the plate using trypsin-EDTA and counted using a Multisizer II.(Only for Reference)

别名	Bazedoxifene HCl, 盐酸巴多昔芬, TSE-424
分子量	507.06
分子式	C30H34N2O3·HCl
CAS No.	198480-56-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: <1 mg/mL

Ethanol: <1 mg/mL

DMSO: 93 mg/mL (183.4 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9722 mL	9.8608 mL	19.7215 mL	49.3038 mL
	5 mM	0.3944 mL	1.9722 mL	3.9443 mL	9.8608 mL
	10 mM	0.1972 mL	0.9861 mL	1.9722 mL	4.9304 mL
	20 mM	0.0986 mL	0.493 mL	0.9861 mL	2.4652 mL
	50 mM	0.0394 mL	0.1972 mL	0.3944 mL	0.9861 mL
	100 mM	0.0197 mL	0.0986 mL	0.1972 mL	0.493 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Miller CP, et al. J Med Chem, 2001, 44(11), 1654-1657. 2. Diane M Biskobing, et al. Clin Interv Aging. 2007 Sep; 2(3): 299–303. 3. Komm BS, et al. Endocrinology, 2005, 146(9), 31999-42008. 4. Li J, Yu F, Guo H, et al. Crystal structure of plant PLDα1 reveals catalytic and regulatory mechanisms of eukaryotic phospholipase D[J]. Cell Research. 2020, 30(1): 61-69.

文献引用

1. Li J, Yu F, Guo H, et al. Crystal structure of plant PLDα1 reveals catalytic and regulatory mechanisms of eukaryotic phospholipase D. Cell Research. 2020, 30(1): 61-69.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Bazedoxifene hydrochloride 198480-56-7 Endocrinology/Hormones Estrogen Receptor/ERR Estrogen/progestogen Receptor interactions TSE424 ERβ IL-6/GP130 STAT3 SERM Inhibitor selective estrogen Bazedoxifene Hydrochloride protein-protein receptor TSE 424 Bazedoxifene HCl ERα modulator 盐酸巴多昔芬 inhibit TSE-424 Bazedoxifene inhibitor

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Bazedoxifene hydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

剂量换算

体内实验配液计算器

技术支持

Keywords