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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / 内皮素受体 / Ambrisentan

安倍生坦 /Ambrisentan {[allProObj[0].p_purity_real_show]}

货号：A121424 同义名： 安贝生坦 / LU 208075;BSF 208075

Ambrisentan is an oral, once-daily endothelin receptor antagonist that is selective for the endothelin type A receptor (IC50s = 0.251, 0.316, 0.398, 251, and 630 nM for rat preparations of heart, bladder, kidney, lung, and cerebral cortex, respectively).

Ambrisentan 化学结构 CAS号：177036-94-1
Ambrisentan 化学结构
CAS号：177036-94-1
Ambrisentan 3D分子结构
CAS号：177036-94-1
Ambrisentan 化学结构 CAS号：177036-94-1
Ambrisentan 3D分子结构 CAS号：177036-94-1
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Ambrisentan 纯度/质量文件 产品仅供科研

货号：A121424 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 ET-A ↓ ET-B ↓ 其他靶点 纯度
BQ-123 +++

Endothelin A receptor, IC50: 7.3 nM

 		98%
Macitentan ++++

ET-A, IC50: 0.5 nM

 		+

ET-B, IC50: 391 nM

 		98%
Zibotentan ++

ET-A, IC50: 21 nM

 		99%+
Bosentan hydrate +++

ET-A, Ki: 4.7 nM

 		++

ET-B, Ki: 95 nM

 		98%
Ambrisentan ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Ambrisentan 生物活性

靶点

  • ET-A
描述 Endothelin-1 (ET-1) is the most predominant isoform of an isopeptides family that has potent vasoconstrictor activity. ET-1 is mediated by two receptor subtypes, endothelin receptor type A (ET<sub>A</sub>) and B (ET<sub>B</sub>). Ambrisentan is a diphenyl propionic acid that acts as a potent ET<sub>A</sub> antagonist. The affinity of ambrisentan for human ET<sub>A</sub> expressed in CHO cells is 1 nM, and the K<sub>i</sub> value of ambrisentan for ET<sub>A</sub> in intact cells expressing human recombinant ET<sub>A</sub> is 0.63 nM. In LS180 cells, the mRNA expressions of CYP3A4, CYP2C9, ABCB1, SLCO1B1, SLCO2B1, PXR were significantly induced by 50 µM ambrisentan after 4-day incubation. The same treatment also resulted in 5.1-fold induction of P-gp expression and 1.2-fold of PXR expression. Ambrisentan at the concentration from 0.1 - 20 µM had a dose-dependent effect on PXP activity in LS180 cells. In OATP1B1 over-expressing cell lines, ambrisentan inhibited intracellular 8-FcA fluorescence with an IC50 value at 27.3 ± 8.6 µM. Ambrisentan (0.1 – 100 nM) showed dose-dependent inhibition on specific [<sup>125</sup>I]ET-1 binding in rat bladder. Nonlinear least-squares regression analysis showed two populations of [<sup>125</sup>I]ET-1 binding sites for ambrisentan, one with high affinity (pIC50 = 9.4 ± 0.7 nM), and the other with low affinity (pIC50 = 7.7 ± 0.5 nM). Moreover, 6 nM ambrisentan increased the K<sub>d</sub> value for specific [<sup>125</sup>I]ET-1 binding in rat bladder 2.32 times compared to that in control group, whereas the effect on the B<sub>max</sub> value was moderate.
作用机制 Ambrisentan is a propionic acid-based selective antagonist for ET<sub>A</sub> that can be orally administrated to treat pulmonary arterial hypertension.

Ambrisentan 动物研究

Dose Rat: 0.1 mg/kg<a href="#ulrefer"><sup>[3]</sup></a> (i.p.); 0.2 mg/kg<a href="#ulrefer"><sup>[4]</sup></a> (p.o.)<br>Danio rerio: 2.5 mg/kg - 5 mg/kg<a href="#ulrefer"><sup>[5]</sup></a> (i.p.)
Administration i.p.

Ambrisentan 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01467791 - Unknown January 2018 United States, Ohio ... 展开 >> University of Cincinnati Recruiting Cincinnati, Ohio, United States, 45267 Contact: Rebecca Ingledue    513-584-6252    ingledra@ucmail.uc.edu    Principal Investigator: Robert P Baughman, MD          Sub-Investigator: Peter Engel, MD 收起 <<
NCT01347216 - Recruiting June 2020 Belgium ... 展开 >> Dept. of Pneumology, University Recruiting Leuven, Belgium Contact: Marion Delcroix, MD, PhD          Principal Investigator: Marion Delcroix, MD, PhD          Germany DRK-Klinikum Köpenick Recruiting Berlin, Germany Contact: Christian Opitz, MD, PhD          Principal Investigator: Christian Opitz, MD, PhD          Lung Centre, University of Giessen Recruiting Giessen, Germany Contact: Ardeschir Ghofrani, MD, PhD          Principal Investigator: Ardeschir Ghofrani, MD          Sub-Investigator: Melanie Thamm, MD          Department of Pulmology; Hannover Medical School Recruiting Hannover, Germany Contact: Marius M Hoeper          Principal Investigator: Marius M Hoeper, MD, PhD          Sub-Investigator: Karen Olsson, MD          German Heart Centre Recruiting Munich, Germany Contact: Harald Kaemmerer, MD,. PhD          Principal Investigator: Harald Kaemmerer, MD, PhD          Ireland Mater Misericordiae Recruiting Dublin, Ireland Contact: Sean Gaine, MD, PhD          Principal Investigator: Sean Gaine, MD, PhD          Italy Department of Cardiovascular and Respiratory Sciences, University La Sapienza Recruiting Rome, Italy Contact: Dario Vizza, MD, PhD          Principal Investigator: Dario Vizza, MD, PhD          Switzerland Dept. for Rheumatology, University Hospital Recruiting Zurich, Switzerland Contact: Oliver Distler, MD, PhD          Principal Investigator: Oliver Distler, MD, PhD 收起 <<
NCT02565030 - Active, not recruiting October 2021 United Kingdom ... 展开 >> Sheffield Teaching Hospitals NHS Foundation Trust Sheffield, South Yorkshire, United Kingdom, S10 2JF 收起 <<

Ambrisentan 参考文献

[1]Yokoyama Y, Osano A, et al. Endothelin-1 receptors in rat tissues: characterization by bosentan, ambrisentan and CI-1020. Biol Pharm Bull. 2014;37(3):461-5.

[2]Weiss J, Herzog M, Haefeli WE. Differential modulation of the expression of important drug metabolising enzymes and transporters by endothelin-1 receptor antagonists ambrisentan and bosentan in vitro. Eur J Pharmacol. 2011 Jun 25;660(2-3):298-304.

[3]Radiloff D, Zhao Y, et al. Anti-hypotensive treatment and endothelin blockade synergistically antagonize exercise fatigue in rats under simulated high altitude. PLoS One. 2014 Jun 24;9(6):e99309.

[4]Lee H, Yeom A, et al. Effect of Ambrisentan Therapy on the Expression of Endothelin Receptor, Endothelial Nitric Oxide Synthase and NADPH Oxidase 4 in Monocrotaline-induced Pulmonary Arterial Hypertension Rat Model. Korean Circ J. 2019 Sep;49(9):866-876.

[5]Muthuraman A, Nafisa K, et al. Role of ambrisentan (selective endothelin-A receptor antagonist) on cigarette smoke exposure induced cognitive impairment in Danio rerio. Life Sci. 2019 Apr 1;222:133-139.

[6]Ambrisentan

Ambrisentan 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.21mL

2.64mL

1.32mL

26.43mL

5.29mL

2.64mL

Ambrisentan 技术信息

CAS号177036-94-1
分子式C22H22N2O4
分子量 378.421
别名 安贝生坦 ;LU 208075;BSF 208075;pulmonext.;Volibris;Ambrisentan. trade name Letairis
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 105 mg/mL(277.47 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 7 mg/mL(18.5 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方

Tags: Ambrisentan | 177036-94-1 | BSF 208075 | LU 208075 | BSF208075 | BSF-208075 | LU208075 | LU 208075 | LU-208075 | Endothelin Receptor Antagonist | GPCR/G Protein | Endothelin Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Ambrisentan 纯度/质量文件 | Ambrisentan 亚型比较 | Ambrisentan 生物活性 | Ambrisentan 动物研究 | Ambrisentan 临床数据 | Ambrisentan 参考文献 | Ambrisentan 实验方案 | Ambrisentan 技术信息

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