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ambrisentan
| 别名 | Letairis® |
|---|---|
| Compound Class | Synthetic organic |
| 变动原因 | Ambrisentan is an endothelin receptor antagonist, with selectivity for the type A endothelin receptor (ETA). |
| Related Product | 安贝生坦 |
Summary
| 是否批准为药物？ | (FDA (2007), EMA (2008)) |
|---|---|
| IUPAC Name | (2S)-2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-di(phenyl)propanoic acid |
| 别名 | Letairis® |
数据库链接
| CAS Registry No. | 177036-94-1 |
|---|---|
| Wikipedia | Ambrisentan |
| PubChem CID | 6918493 |
| ChEMBL Ligand | CHEMBL1111 |
| ChEBI | CHEBI:254051 |
| PEP | ambrisentan |
| DrugCentral Ligand | 4337 |
| GPCRdb Ligand | 3951 |
生物活性
| 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 |
|---|---|
| 关联靶标 | ETA receptor , ETA receptor , ETB receptor |
临床资料
| Summary of Clinical Use |
Approved to treat pulmonary arterial hypertension (PAH). Ambrisentan is being evaluated in Phase 3 clinical trial for the additional indication chronic thromboembolic pulmonary hypertension. COVID-19: In response to the SARS-CoV-2 pandemic, clinical trials were initiated to address the potential of endothelin receptor antagonism as a treatment for endothelial cell damage and dysfunction in the blood vessels (in the lungs and other organs) that occurs during SARS-CoV-2 infection. |
|---|---|
| 作用机制与药效学效应 | Ambrisentan is a selective endothelin receptor A (ETA) antagonist. Antagonism of endothelin binding to ETA decreases vasoconstriction in the smooth muscle of the lungs and reduces pulmonary blood pressure. |
结构
| Canonical SMILES | COC(C(C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 |
|---|---|
| Isomeric SMILES | COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 |
| 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 |
危险品化学品经营许可证（带存储）