95094-00-1
中文名稱
卡維地絡雜質B
英文名稱
(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 結構式
基本信息
中文別名
(S)-卡維地洛卡維地洛S-異構體
英文別名
(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)-
物理化學性質
熔點114-115°C
沸點655.2±55.0 °C(Predicted)
密度1.250±0.06 g/cm3(Predicted)
儲存條件-20°C冷凍
酸度系數(pKa)13.90±0.20(Predicted)
應用領域
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.常見問題列表
生物活性
(S)-Carvedilol 是 Carvedilol 的 S 型異構體，是一種非選擇性 β/α-1 受體阻斷劑。(S)-Carvedilol 可以抵抗 Doxorubicin (DOX) 的血管或心臟毒性。靶點
β/α-1 adrenergic receptor
體外研究
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.