171714-84-4
中文名称
达卢生坦
英文名称
Darusentan
CAS
171714-84-4
分子式
C22H22N2O6
分子量
410.42
MOL 文件
171714-84-4.mol
更新日期
2025/11/25 15:12:05
171714-84-4 结构式
基本信息
中文别名
达卢生坦(S)-2-((4,6-二甲氧基嘧啶-2-基)氧基)-3-甲氧基-3,3-二苯丙酸
英文别名
HMR4005HMR-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
物理化学性质
沸点587.3±60.0 °C(Predicted)
密度1.268±0.06 g/cm3(Predicted)
储存条件Sealed in dry,2-8°C
溶解度DMF: 10 mg/ml; DMSO: 2 mg/ml; Ethanol: 2 mg/ml; PBS (pH 7.2): insol
酸度系数(pKa)1.82±0.10(Predicted)
形态固体
颜色White to off-white
达卢生坦价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/09/19 | S0017 | 达卢生坦 Lu-135252 | 171714-84-4 | 5mg | 2514.33元 |
| 2025/09/19 | S0017 | 达卢生坦 Lu-135252 | 171714-84-4 | 25mg | 7608.51元 |
| 2025/05/22 | HY-15404 | 达卢生坦 Darusentan | 171714-84-4 | 1 mg | 495元 |
常见问题列表
生物活性
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。体外研究
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.
体内研究
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.
| Animal Model: | Twenty-four (eight per group) male Sprague Dawley rats weighing 175±200 g |
| Dosage: | 30 mg/kg |
| Administration: | Administered orally in rat food for weeks 3 and 4 |
| Result: | Reversed aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg). |