达卢生坦
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- CAS号:
- 171714-84-4
- 英文名:
- Darusentan
- 英文别名:
- HMR4005;HMR 4005;HMR-4005;Darusentan;S-Darusentan;darusentan, CID177236;FEJVSJIALLTFRP-LJQANCHMSA-N;LU 135252; LU-135252; LU135252; HMR-4005; HMR 4005; HMR4005; DARUSENTAN;(S)-2-((4,6-dimethoxypyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropanoic acid;(2S)-2-(4,6-DIMETHOXYPYRIMIDIN-2-YL)OXY-3-METHOXY-3,3-DI(PHENYL)PROPANOIC ACID
- 中文名:
- 达卢生坦
- 中文别名:
- 达卢生坦;达尔斯坦坦;(S)-2-((4,6-二甲氧基嘧啶-2-基)氧基)-3-甲氧基-3,3-二苯丙酸
- CBNumber:
- CB42485038
- 分子式:
- C22H22N2O6
- 分子量:
- 410.42
- MOL File:
- 171714-84-4.mol
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达卢生坦化学性质
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沸点:
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587.3±60.0 °C(Predicted)
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密度:
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1.268±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMF: 10 mg/ml; DMSO: 2 mg/ml; Ethanol: 2 mg/ml; PBS (pH 7.2): insol
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形态:
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A solid
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酸度系数(pKa):
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1.82±0.10(Predicted)
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颜色:
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White to off-white
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达卢生坦性质、用途与生产工艺
Darusentan (Lu-135252) 是一种选择性内皮素受体 A (ET-A) 受体拮抗剂，其与 ET-A 受体的 Ki 为 1.4 nM，与 ET-B 受体的 Ki 为 184 nM，对 ETA 受体的选择性比 ETB 受体高100多倍。Darusentan 在大鼠主动脉血管平滑肌细胞 (RAVSMs) 膜中竞争结合放射性标记的内皮素，Ki 为 13 nM。
Darusentan ((S)-Darusentan) competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a K
i
=13 nM. In isolated endothelium-denuded rat aortic rings, Darusentan inhibits endothelin-induced vascular contractility with a pA
2
=8.1±0.14. Darusentan ( 0.001-1μM) inhibits ET-1-induced signaling in cultured RAVSMs.
Darusentan (30 mg/kg per day orally for weeks 3 and 4) reverses aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg per min subcutaneously for 2 and 4 weeks) in male Sprague Dawley rats.
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Animal Model:
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Twenty-four (eight per group) male Sprague Dawley rats weighing 175±200 g
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Dosage:
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30 mg/kg
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Administration:
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Administered orally in rat food for weeks 3 and 4
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Result:
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Reversed aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg).
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达卢生坦
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/08/19 | HY-15404 | Darusentan | | 1 mg | 495元 |
| 2024/08/19 | HY-15404 | 达卢生坦
Darusentan | 171714-84-4 | 5mg | 1300元 |
171714-84-4, 达卢生坦 相关搜索:
- 合成有机化合物配体
- 达尔斯坦坦
- (S)-2-((4,6-二甲氧基嘧啶-2-基)氧基)-3-甲氧基-3,3-二苯丙酸
- 达卢生坦
- 171714-84-4
- vascular,ET-A,Darusentan,Endothelin Receptor,rat,muscle,Inhibitor,Lu 135252,receptor,aortic,endothelin,inhibit,smooth,RAVSMs,Lu135252
- Benzenepropanoic acid, α-[(4,6-dimethoxy-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-, (αS)-
- FEJVSJIALLTFRP-LJQANCHMSA-N
- darusentan, CID177236
- (2S)-2-(4,6-DIMETHOXYPYRIMIDIN-2-YL)OXY-3-METHOXY-3,3-DI(PHENYL)PROPANOIC ACID
- LU 135252; LU-135252; LU135252; HMR-4005; HMR 4005; HMR4005; DARUSENTAN
- HMR-4005
- HMR4005
- HMR 4005
- S-Darusentan
- (S)-2-((4,6-dimethoxypyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropanoic acid
- Darusentan