171714-84-4
中文名稱
達(dá)盧生坦
英文名稱
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
2024/07/08 16:38:17
171714-84-4 結(jié)構(gòu)式
基本信息
中文別名
達(dá)盧生坦(S)-2-((4,6-二甲氧基嘧啶-2-基)氧基)-3-甲氧基-3,3-二苯丙酸
英文別名
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
物理化學(xué)性質(zhì)
沸點(diǎn)587.3±60.0 °C(Predicted)
密度1.268±0.06 g/cm3(Predicted)
儲(chǔ)存條件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
酸度系數(shù)(pKa)1.82±0.10(Predicted)
形態(tài)固體
顏色White to off-white
常見問題列表
生物活性
Darusentan (Lu-135252) 是一種選擇性內(nèi)皮素受體 A (ET-A) 受體拮抗劑，其與 ET-A 受體的 Ki 為 1.4 nM，與 ET-B 受體的 Ki 為 184 nM，對(duì) ETA 受體的選擇性比 ETB 受體高100多倍。Darusentan 在大鼠主動(dòng)脈血管平滑肌細(xì)胞 (RAVSMs) 膜中競(jìng)爭(zhēng)結(jié)合放射性標(biāo)記的內(nèi)皮素，Ki 為 13 nM。體外研究
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.
體內(nèi)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). |