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Ambrisentan

Ambrisentan

产品编号 T1655   CAS 177036-94-1
别名: BSF-208075, BSF 208075, 安倍生坦, LU 208075

Ambrisentan (BSF 208075) 是 ET A 型受体选择性拮抗剂。

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Ambrisentan Chemical Structure
Ambrisentan, CAS 177036-94-1
规格 价格/CNY 货期 数量
1 mg ¥ 191 现货
5 mg ¥ 413 现货
10 mg ¥ 622 现货
25 mg ¥ 982 现货
50 mg ¥ 1,580 现货
100 mg ¥ 2,380 现货
500 mg ¥ 5,680 现货
1 mL * 10 mM (in DMSO) ¥ 455 现货
其他形式的 Ambrisentan:
产品目录号及名称: Ambrisentan (T1655)
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纯度: 99.85%
纯度: 99.65%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Ambrisentan (BSF 208075) is an endothelin receptor antagonist used in the therapy of pulmonary arterial hypertension (PAH). Ambrisentan has been associated with a low rate of serum enzyme elevations during therapy but has yet to be implicated in cases of clinically apparent acute liver injury.
体内活性 Hepatic hydroxyproline content in the Ambrisentan group is significantly lower compared to the control group (18.0 μg/g±6.1 μg/g vs 33.9 μg/g±13.5 μg/g liver, respectively, P=0.014). Hepatic fibrosis estimated by Sirius red staining and areas positive for α-smooth muscle actin, indicative of activated hepatic stellate cells, are also significantly lower in the Ambrisentan group (0.46%±0.18% vs 1.11%±0.28%, respectively, P=0.0003; and 0.12%±0.08% vs 0.25%±0.11%, respectively, P=0.047). In addition, hepatic RNA expression levels of procollagen-1 and tissue inhibitor of metalloproteinase-1 (TIMP-1) are significantly lower by 60% and 45%, respectively, in the Ambrisentan group. Inflammation, steatosis, and endothelin-related mRNA expression in the liver are not significantly different between the groups. Ambrisentan attenuates the progression of hepatic fibrosis by inhibiting hepatic stellate cell activation and reducing procollagen-1 and TIMP-1 gene expression. Ambrisentan did not affect inflammation or steatosis[6].
激酶实验 In vitro PTPase assays: Individual PTPases (0.01 μg/reaction) in 50 μL of PTPase buffer [50 mM Tris (pH 7.4)] are incubated at 22 ℃ for 10 min or as indicated in the absence or presence of inhibitory compounds. Substrates (0.2 mM phosphotyrosine peptide) are then added and allows to react at 22 ℃ for 18 hr. PTPase activity of individual reactions is measured by adding 100 μL of malachite green solution (UBI) and then quantifying the amounts of free phosphate cleaved by the PTPase from the peptide substrate by spectrometry (A660 nm). Relative PTPase activities are calculated based on the formula [(PTPase activity in the presence of an inhibitory compound)/(PTPase activity in the absence of the compound) &times 100%]. Reactions performed under comparable conditions in the absence of recombinant PTPases only are used as controls and shows no detectable PTPase activity.
细胞实验 Ambrisentan is dissolved in DMSO and stored, and then diluted with appropriate medium before use. Unless otherwise stated, for each BMEC experiment cells are randomly divided into 4 groups: (1) normoxia vehicle control (Nx-CTRL); (2) normoxia-treated; (3) hypoxia (24 h) control (Hx-CTRL) and (4) hypoxia (24 h) treated. As previously described, Nrf2 activators are added 24 h prior to any hypoxic exposures. Cell treatments are; Protandim (100 μg/mL), methazolamide (125 μg/mL, nifedipine (7 μg/mL) or Ambrisentan (40 μg/mL). In addition, some cells are treated with Nrf2 siRNA. In these experiments, siRNA is added 24 h prior to drug treatments. The rationale for 24 h hypoxia exposure for BMEC is to ensure that cells remained transfected with siRNA for the pre-treatment of drugs (24 h in normoxia) and during the 24 h hypoxia exposure. Data is collected from at least three separate cell culture preparations on three separate days (n=9)[2].
别名 BSF-208075, BSF 208075, 安倍生坦, LU 208075
分子量 378.42
分子式 C22H22N2O4
CAS No. 177036-94-1

存储

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

溶解度

Ethanol: 6 mg/mL(15.9 mM)

DMSO: 71 mg/mL (187.6 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.6426 mL 13.2128 mL 26.4257 mL 66.0642 mL
5 mM 0.5285 mL 2.6426 mL 5.2851 mL 13.2128 mL
10 mM 0.2643 mL 1.3213 mL 2.6426 mL 6.6064 mL
DMSO 20 mM 0.1321 mL 0.6606 mL 1.3213 mL 3.3032 mL
50 mM 0.0529 mL 0.2643 mL 0.5285 mL 1.3213 mL
100 mM 0.0264 mL 0.1321 mL 0.2643 mL 0.6606 mL

计算器

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配液计算器
分子量计算器
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参考文献

1. Weiss J, et al. Eur J Pharmacol,2011, 660(2-3), 298-304. 2. Yokoyama Y, et al. Biol Pharm Bull,2014, 37(3), 461-465. 3. Weiss J, et al. Biochem Pharmacol,2013, 85(2), 265-273. 4. Osano A, et al. J Pharmacol Sci,2014, 124(1), 86-91. 5. Buckley MS, et al. Expert Opin Drug Metab Toxicol,2011, 7(3), 371-380. 6. Okamoto T, et al. Antifibrotic effects of Ambrisentan, an endothelin-A receptor antagonist, in a non-alcoholic steatohepatitis mouse model. World J Hepatol. 2016 Aug 8;8(22):933-41.
Avosentan Macitentan Aminaftone BMS 182874 Ro 46-2005 Edonentan Sulfisoxazole Atrasentan hydrochloride

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 抗癌上市药物库 抗癌药物库 抗癌临床化合物库 抗心血管疾病化合物库 抗癌化合物库 FDA上市及药典收录分子库 内分泌激素分子库 神经递质受体化合物库 抑制剂库

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
g
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。
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% ddH2O
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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

Ambrisentan 177036-94-1 GPCR/G Protein Endothelin Receptor inhibit BSF-208075 BSF 208075 安倍生坦 LU-208075 BSF208075 Inhibitor LU208075 LU 208075 inhibitor

 

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