Ys-49

Biological Activity

YS 49 inhibits Ang II-stimulated proliferation of VSMCs via induction of HO-1.YS-49 is a novel positive inotropic isoquinoline compound. YS-49 has potential as a therapeutic strategy for the pathogenesis of Ang II-related vascular diseases such as hypertension and atherosclerosis, via the induction of HO-1 gene activity. YS-49 induced HO-1 protein production in a dose-and time-dependent manner in VSMCs. Treatment with YS-49 significantly and dose-dependently inhibited Ang II-induced VSMC proliferation, ROS production, and phosphorylation of JNK, but not P38 MAP kinase or ERK1/2.YS-49(32.8 microM) exhibited much stronger inhibitory effects on TXA(2) formation. The higher inhibitory potencies of YS-49 (IC(50): 3.3microM) than higenamine (IC(50): 140 microM) on AA induced rat platelet aggregation was presumed to be the result of low inhibitory effect of higenamine than YS-49 on TXA(2) production from AA. The oral administration of YS-49 (50 mg/kg) increased the recovery rates from the acute thrombotic challenge in mice and lowered the weight of thrombus formed inside the AV shunt tube in rats.

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.