| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A408058-1ml |
1ml |
现货  |
|
| 英文别名 | LU-208075, BSF-208075 | (αS)-α-[(4,6-dimethyl-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-benzenepropanoic acid |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Ambrisentan |
| 生化机理 | 安利生坦（LU-208075，BSF-208075）是一种高选择性内皮素-1 A 型受体拮抗剂，用于治疗肺动脉高压（PAH）。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 拮抗剂 |
| 作用机制 | 内皮素受体，ET-A/ET-B 拮抗剂 |
| 产品介绍 |
Ambrisentan is a selective ET type A receptor (ETAR) antagonist. Information Ambrisentan Ambrisentan (LU-208075, BSF-208075) is a highly selective antagonist of the endothelin-1 type A receptor , used in the treatment of pulmonary arterial hypertension (PAH). Ambrisentan only increases intracellular calcein fluorescence in P388/dx cells at concentrations above 100 μM and in L-MDR1 cells not at all indicating negligible P-gp inhibition. Ambrisentan inhibits specific [(125)I]ET-1 binding in these tissues in a concentration-dependent manner. Ambrisentan undergoes oxidative metabolism mainly by cytochrome P450 (CYP) 3A4 and to a lesser extent by CYP3A5 and CYP2C19. Ambrisentan is not only a strong inducer of CYP3A4, but also of ABCB1 and ABCG2. Ambrisentan also has a concentration-dependent effect on PXR activity, but because plateau effects are not reached, an EC50-value could not be calculated. Ambrisentan inhibits specific [(125)I]ET-1 binding in a concentration-dependent manner at nanomolar ranges of IC50. Ambrisentan significantly increases the dissociation constant for bladder [(125)I]ET-1 binding without affecting maximal number of binding sites (Bmax). Ambrisentan seem to bind to bladder ET-1 receptor in a competitive and reversible manner. Ambrisentan is an effective and safe treatment which is a valuable addition to the armamentarium against PAH. Ambrisentan offers a relative lack of drug interactions, once daily dosing and reassuring liver safety, offering safety and convenience advantages over bosentan. In vivo
cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 3.659 |
|---|---|
| hba_count | 5 |
| Rotatable Bond | 7 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC(C(OC1=NC(=CC(=N1)C)C)C(O)=O)(C2=CC=CC=C2)C3=CC=CC=C3 |
| 分子量 | 378.42 |
| Reaxy-Rn | 7549073 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7549073&ln= |
| DMSO(mg / mL) Max Solubility | 76 |
|---|---|
| DMSO(mM) Max Solubility | 200.84 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 7549073 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7549073&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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