ZLN005, CAS NO.49671-76-3

zln005 is a novel transcriptional regulator of peroxisome proliferator-activated receptor-γ coactivator-1α (pgc-1α).
ic50 value:
target: pgc-1α
in vitro: zln005 increases expression of the pgc-1α gene in l6 myotubes. zln005 increased pgc-1α mrna levels in a dose-dependent manner; 20 μmol/l zln005 caused a threefold increase over the control after 24 h. at 10 μmol/l, the pgc-1α mrna levels were increased to almost the same extent at 16 to 48 h [1]. zln005 did not increase the expression of the pgc-1α gene in rat primary hepatocytes. amp-activated protein kinase is involved in the mechanism inducing pgc-1α in l6 myotubes [1]
in vivo: an insulin tolerance test revealed that treatment with zln005 significantly decreased insulin resistance in db/db mice, as evidenced by the approximately 18% decrease in the auc. a ptt also was performed in db/db mice, and zln005 improved pyruvate tolerance, as evidenced by the 16% decrease in the auc. in db/db mice, plasma nefa and triglyceride levels were decreased by 20% and 37%, respectively, and cholesterol was decreased by 10% with zln005 treatment. plasma insulin and β-hydroxybutyrate content, liver/bodyweight index and adipose composition, and muscle and liver triglyceride levels, however, were not ameliorated by treatment with zln005 or metformin [1].