Aprocitentan (ACT-132577)
产品编号: DC11513
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应用领域
Aprocitentan (ACT-132577) 是 Macitentan 的主要活性代谢物。Aprocitentan 是双重 ETA/ETB 拮抗剂，IC50 分别为 3.4 nM 和 987 nM，pA2 值分别为 6.7 和 5.5。
| Cas No.: |
1103522-45-7 |
| 名称: |
N-[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]sulfuric diamide |
| 别名: |
Aprocitentan; ACT-132577; ACT 132577; ACT132577; Despropyl Macitentan |
| SMILES: |
O=S(NC1=NC=NC(OCCOC2=NC=C(Br)C=N2)=C1C3=CC=C(Br)C=C3)(N)=O |
| 分子式: |
C16H14Br2N6O4S |
| 分子量: |
546.19 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| References: |
Aprocitentan, also known as ACT-132577, is an endothelin receptor antagonist and an pharmacologically active metabolite of macitentan (MedKoo Cat#205912). Aprocitentan antagonized the specific binding of ET-1 on membranes of cells overexpressing ET(A) and ET(B) receptors and blunted ET-1-induced calcium mobilization in various natural cell lines, with inhibitory constants within the nanomolar range. |
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MSDS
COA
| LOT NO. |
DOWNLOAD |
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| 2018-0101 |
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询盘
