达卢生坦

生物活性体外研究体内研究达卢生坦试剂级价格

达卢生坦

CAS号:171714-84-4
英文名:Darusentan
中文名:达卢生坦
CBNumber:CB42485038
分子式:C22H22N2O6
分子量:410.42
MOL File:171714-84-4.mol

达卢生坦化学性质

沸点 :587.3±60.0 °C(Predicted)
密度 :1.268±0.06 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMF: 10 mg/ml; DMSO: 2 mg/ml; Ethanol: 2 mg/ml; PBS (pH 7.2): insol
形态 :A solid
酸度系数(pKa) :1.82±0.10(Predicted)
颜色 :White to off-white

达卢生坦性质、用途与生产工艺

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).