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安贝生坦

选择性ETA拮抗剂
规格或纯度: ≥99%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
A126631-10mg 10mg 现货 Stock Image
A126631-25mg 25mg 现货 Stock Image
A126631-100mg 100mg 现货 Stock Image
A126631-250mg 250mg 现货 Stock Image
A126631-1g 1g 期货 Stock Image
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ETA receptor Antagonist ETB receptor Antagonist
main product photo

基本描述

规格或纯度 ≥99%
英文名称 Ambrisentan
别名 安贝生坦；安倍生坦；(S)-2-[(4,6-二甲基嘧啶-2-基)氧]-3-甲氧基-3,3-二苯基丙酸；凡瑞克
英文别名 (+)-(2S)-2-[(4，6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3，3-diphenylpropanoic acid;(S)-2-[(4,6-Dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropionic Acid
生化机理 选择性内皮素受体ETA拮抗剂。显示ETAover ETB的选择性约为200倍（Ki值分别为1 nM和195 nM）。预防内皮素诱发的大鼠猝死。
储存温度 2-8°C储存
运输条件 冰袋运输
产品介绍

Ambrisentan is a?selective ET type A?receptor (ETAR) antagonist.

Ambrisentan is a?selective ET type A?receptor (ETAR) antagonist.

名称和标识符

IUPAC Name (2S)-2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid
INCHI InChI=1S/C22H22N2O4/c1-15-14-16(2)24-21(23-15)28-19(20(25)26)22(27-3,17-10-6-4-7-11-17)18-12-8-5-9-13-18/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1
InChi Key OUJTZYPIHDYQMC-LJQANCHMSA-N
Canonical SMILES CC1=CC(=NC(=N1)OC(C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)C
分子式

C22H22N2O4
PubChem CID 6918493
分子量 378.42

化学和物理性质

溶解性 溶于DMSO, 最高浓度 (mg/mL): 37.84, 最高浓度(mM): 100；溶于ethanol, 最高浓度 (mg/mL): 37.84, 最高浓度(mM): 100
熔点 178 °C(dec.)
比旋光度 173° (C=0.5,MeOH)

安全信息

象形图
ghs08

Health Hazard
信号词 Danger
危险声明 H351: Suspected of causing cancer
H372: Causes damage to organs through prolonged or repeated exposure
H361: Suspected of damaging fertility or the unborn child
H360FD: May damage fertility; May damage the unborn child
预防措施声明 P280,P405,P501,P264,P260,P270,P203,P318,P319
RTECS UA2459660
Merck Index 384

靶标

Target ID 219
名称 ETA receptor
缩写名 SHP2
家族 Endothelin receptors
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Rat 7 426 19q11 Ednra endothelin receptor type A
Human 7 427 4q31.22-q31.23 EDNRA endothelin receptor type A
Mouse 7 427 8 C1 Ednra endothelin receptor type A
RefSeq Protein NP_036682 (Rn) , NP_001948 (Hs) , NP_034462 (Mm)
UniProtKB P26684 (Rn) , P25101 (Hs) , Q61614 (Mm)
OMIM 131243 (Hs)
RefSeq Nucleotide NM_001957 (Hs) , NM_012550 (Rn) , NM_010332 (Mm)
Entrez Gene 1909 (Hs) , 24326 (Rn) , 13617 (Mm)
Ensembl Gene ENSG00000151617 (Hs) , ENSMUSG00000031616 (Mm) , ENSRNOG00000012721 (Rn)
Protein GI 372266194 (Hs) , 45383740 (Mm) , 7549758 (Rn)
GPCRdb ednra_human (Hs) , ednra_mouse (Mm) , ednra_rat (Rn)
UniProtKB ID/Entry name EDNRA_HUMAN (Hs) , EDNRA_MOUSE (Mm) , EDNRA_RAT (Rn)
DrugBank Target P25101 (Hs)
ChEMBL Target CHEMBL4566 (Rn) , CHEMBL2286 (Mm) , CHEMBL252 (Hs)
Target ID 220
名称 ETB receptor
缩写名 SHP2
家族 Endothelin receptors
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Rat 7 442 15q22 Ednrb endothelin receptor type B
Human 7 442 13q22.3 EDNRB endothelin receptor type B
Mouse 7 442 14 53.05 cM Ednrb endothelin receptor type B
RefSeq Protein NP_059029 (Rn) , NP_000106 (Hs) , NP_031930 (Mm)
UniProtKB P21451 (Rn) , P24530 (Hs) , P48302 (Mm)
OMIM 131244 (Hs)
RefSeq Nucleotide NM_000115 (Hs) , NM_017333 (Rn) , NM_007904 (Mm)
Entrez Gene 1910 (Hs) , 50672 (Rn) , 13618 (Mm)
Ensembl Gene ENSG00000136160 (Hs) , ENSMUSG00000022122 (Mm) , ENSRNOG00000010997 (Rn)
Orphanet 121287 (Hs)
Protein GI 319655697 (Hs) , 209862929 (Mm) , 8393333 (Rn)
GPCRdb ednrb_human (Hs) , ednrb_mouse (Mm) , ednrb_rat (Rn)
UniProtKB ID/Entry name EDNRB_HUMAN (Hs) , EDNRB_MOUSE (Mm) , EDNRB_RAT (Rn)
DrugBank Target P24530 (Hs)
ChEMBL Target CHEMBL4631 (Rn) , CHEMBL1785 (Hs) , CHEMBL1681617 (Mm)

关联配体

Ligand ID 3951
名称 ambrisentan
别名 Letairis®
类别 Synthetic organic
学名 (2S)-2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-di(phenyl)propanoic acid
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Ambrisentan is an endothelin receptor antagonist, with selectivity for the type A endothelin receptor (ETA).
临床描述 TACTIC-E is a randomised, parallel arm, open-label platform trial for investigating potential treatments for COVID-19 disease. While SARS-CoV infection evades detection by the immune system in the first 24 hours of infection, it ultimately produces a massive immune system response in the subgroup of people who develop severe complications. Most tissue damage following infection with COVID-19 appears to be due to a later, exaggerated, host immune response (Gralinski and Baric 2015). This leads to lung and sometimes multi-organ damage. Most people who develop these severe complications still have virus present in their respiratory tract at the time-point when the disease starts to evolve. Immune modulation in the presence of active infection has potential to cause more harm than benefit. Safety considerations when studying immune modulation strategies are paramount. This study will assess the efficacy of a novel immunomodulatory agent and a novel combination of approved agents which may protect the patient against end-organ damage and modulate the pulmonary vascular response. This study will compare the novel therapeutic agent EDP1815 and a novel combination of the approved agents dapagliflozin and ambrisentan against Standard of Care.
Patients with COVID-19 frequently develop lower respiratory complications. Difficulty breathing and a low concentration of oxygen in the blood are of concern in patients with COVID-19, as they indicate that the lungs may be significantly affected. In some patients, respiratory symptoms may progress to the point where oxygen support is needed (i.e. use of an oxygen prongs, mask or ventilator). The exact mechanism of why patients with COVID-19 develop low concentrations of oxygen in blood is not fully understood. Some data suggest that the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), the virus causing Coronavirus Disease 2019 (COVID-19), can affect the body's blood vessels directly and extensively. In the lung, blood vessels participate in the absorption of oxygen. Endothelin is a potent hormone produced by human blood vessels. When increased, endothelin can result in the narrowing of blood vessels in the lung and decrease the volume of blood flowing through the lungs. This decrease in in blood flow through the lungs may be one of many factors affecting normal lung function. Ambrisentan can block the effects of endothelin in the body, and this could theoretically improve blood flow through the lungs. This study will evaluate whether ambrisentan, by blocking the effects of the hormone endothelin in the lungs, improves the breathing capacity of patients with COVID-19, increases the concentration of oxygen in the blood and prevents the progression to respiratory failure and death. Ambrisentan is a drug that is currently used to treat patients with pulmonary hypertension, a disease where blood flow through the lungs is decreased. Subjects participating in this study are those patients hospitalised with severe respiratory symptoms related to COVID-19, and are considered to be at high-risk of developing respiratory complications. Ambrisentan will be administered in the hospital, and will be continued at home for up to 28 days. In this study, ambrisentan will be administered at much lower doses that those used in patients with pulmonary hypertension.
来源公司 Cambridge University Hospitals NHS Foundation Trust
Noorik Biopharmaceuticals AG

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