95094-00-1
中文名称
卡维地络杂质B
英文名称
(S)-(-)-CARVEDILOL
CAS
95094-00-1
分子式
C24H26N2O4
分子量
406.47
MOL 文件
95094-00-1.mol
更新日期
2024/04/16 10:57:56
95094-00-1 结构式
基本信息
中文别名
(S)-卡维地洛卡维地洛S-异构体
英文别名
(S)-(-)-CARVEDILOLCarvedilol S-IsoMer
(-)-1-(9H-CARBAZOL-4-YLOXY)-3-[[2-(2-METHOXYPHENOXY)ETHYL]AMINO]-2-PROPANOL
(S)-1-(9H-Carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol
(2S)-1-(9H-Carbazole-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]propane-2-ol
[S,(-)]-1-(9H-Carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol
2-Propanol, 1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-, (S)-
2-Propanol, 1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-, (2S)-
物理化学性质
熔点114-115°C
沸点655.2±55.0 °C(Predicted)
密度1.250±0.06 g/cm3(Predicted)
储存条件-20°C冷冻
酸度系数(pKa)13.90±0.20(Predicted)
应用领域
用途1
The optically active isomer of Carvedilol (C184625), a nonselective 脽-adrenergic blocker with a1-blocking activity. An antihypertensive used in the treatment of congestive heart failure.常见问题列表
生物活性
(S)-Carvedilol 是 Carvedilol 的 S 型异构体，是一种非选择性 β/α-1 受体阻断剂。(S)-Carvedilol 可以抵抗 Doxorubicin (DOX) 的血管或心脏毒性。靶点
β/α-1 adrenergic receptor
体外研究
The β-receptor blocking activity of (S)-Carvedilol is about 100 times greater than that of (R)-Carvedilol, whereas both enantiomers show equipotent potency as α-blockers.
(S)-Carvedilol significantly attenuates Doxorubicin (DOX)-induced cell death, apoptotic morphological changes, decrease the mitochondrial membrane potential and oxidative stress responses by increasing the superoxide dismutase and catalase activities, and decreasing malondialdehyde contents and reactive oxygen species levels via the PI3K/AKT/eNO synthase pathway in vitro.
(S)-Carvedilol treatment significantly upregulates the expression levels of p-eNOS in HUVECs.