(S)-Carvedilol is a non-selective β/α-1 blocker.It exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).

(S)-Carvedilol is about 100 times greater than that of (R)-Carvedilol in β-receptor blocking activity, whereas both enantiomers show equipotent potency as α-blockers. (S)-Carvedilol treatment significantly upregulates the expression levels of p-eNOS in HUVECs. (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.