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Bazedoxifene hydrochloride

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产品编号 T6404Cas号 198480-56-7
别名 WAY 140424 hydrochloride, TSE-424 hydrochloride, TSE424 hydrochloride, TSE 424 hydrochloride

Bazedoxifene hydrochloride (TSE 424 hydrochloride) 是一种能透过血脑屏障且具有口服活性、选择性和高效性的雌激素受体调节剂 (SERM),也是 IL-6/GP130 蛋白相互作用抑制剂,对 ERα 和 ERβ 具有很高的亲和力,可用于研究绝经后骨质疏松症和血管舒缩相关疾病。

Bazedoxifene hydrochloride

Bazedoxifene hydrochloride

Rating icon 很棒
纯度: 98.74%
产品编号 T6404 别名 WAY 140424 hydrochloride, TSE-424 hydrochloride, TSE424 hydrochloride, TSE 424 hydrochlorideCas号 198480-56-7

Bazedoxifene hydrochloride (TSE 424 hydrochloride) 是一种能透过血脑屏障且具有口服活性、选择性和高效性的雌激素受体调节剂 (SERM),也是 IL-6/GP130 蛋白相互作用抑制剂,对 ERα 和 ERβ 具有很高的亲和力,可用于研究绝经后骨质疏松症和血管舒缩相关疾病。

规格价格库存数量
1 mg
¥ 492
现货
5 mg
¥ 1,270
现货
10 mg
¥ 2,300
现货
25 mg
¥ 3,590
现货
50 mg
¥ 5,680
现货
100 mg
¥ 7,690
现货
500 mg
¥ 15,300
现货
1 mL x 10 mM (in DMSO)
¥ 1,980
现货
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纯度:98.74%
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产品介绍

生物活性
产品描述
Bazedoxifene hydrochloride (TSE 424 hydrochloride) is an orally active, selective, and potent estrogen receptor modulator (SERM) that crosses the blood-brain barrier and is an inhibitor of IL-6/GP130 protein interactions with high affinity for ERα and ERβ. It has a high affinity for ERα and ERβ and can be used to study postmenopausal osteoporosis and vasodilator-related diseases.
靶点活性
ERβ (rat):99 nM, ERβ:89 nM, ERα:26 nM, ERα:23 nM
体外活性
在 AsPC-1 细胞中,Bazedoxifene hydrochloride(10 μM-20 μM;2 小时)能够抑制由 IL-6、IL-11 或 OSM(各50 ng/mL)诱导的 STAT3 磷酸化[2]。
体内活性
在 6 周龄的雌性无胸腺裸鼠中,Bazedoxifene hydrochloride(剂量为5 mg/kg;通过口服灌胃,每日一次,持续 18 天)被用于抑制胰腺癌异种移植瘤的生长,并在肿瘤细胞中诱导凋亡[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WAY 140424 hydrochloride, TSE-424 hydrochloride, TSE424 hydrochloride, TSE 424 hydrochloride
化学信息
分子量507.06
分子式C30H35ClN2O3
CAS No.198480-56-7
SmilesCl.OC=1C=CC(=CC1)C2=C(C3=CC(O)=CC=C3N2CC4=CC=C(OCCN5CCCCCC5)C=C4)C
密度no data available
储存&溶解度
存储store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: <1 mg/mL
Ethanol: <1 mg/mL
DMSO: 93 mg/mL (183.41 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM1.9722 mL9.8608 mL19.7215 mL98.6077 mL
5 mM0.3944 mL1.9722 mL3.9443 mL19.7215 mL
10 mM0.1972 mL0.9861 mL1.9722 mL9.8608 mL
20 mM0.0986 mL0.4930 mL0.9861 mL4.9304 mL
50 mM0.0394 mL0.1972 mL0.3944 mL1.9722 mL
100 mM0.0197 mL0.0986 mL0.1972 mL0.9861 mL

SCI 文献

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

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
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2 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

剂量转换

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