CMX-2043 is a novel analogue of α-Lipoic Acid ( HY-N0492 ). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase , soluble tyrosine kinase , and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model
In Vitro
CMX-2043 (15-250 mM; 10 min) has great peroxyl radical absorbance capacity. CMX-2043 (1.5 μM) weakly inhibits spleen tyrosine kinase (Syk) and tunica interna endothelial cell kinase (Tie2). CMX-2043 (50 μM; 45 min) activates Akt phosporylation via PI3K pathway in A549 cells. CMX-2043 (2.5 mM; 30 min) diminishes the rise in cytosolic calcium in a concentration-dependent manner in CHO-M1-WT3 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. ImmunofluorescenceCell Line: H9c2 (rat cardiac myocyte) cells Concentration: 50 μM Incubation Time: 3 hours Result: Showed brighter luorescence intensity in cells compared with control, indicating a stronger Akt phosphorylation effect.
In Vivo
CMX-2043 (50-200 mg/kg, 5 mL; p.o.; single dose) reduces myocardial ischemia-reperfusion injury (IRI) as measured by the myocardial infarct to area at risk (MI-AR) ratio and the incidence of arrhythmia. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Ischemia-reperfusion injury (IRI) model in Sprague Dawley ratsDosage: 50, 100, and 200 mg/kg; 5 mL of normal saline solution containing 2% vanilla extract as flavoring Administration: Oral gavage; single dose; induced IRI 30-60 min after treatment Result: Induced arrhythmia and mortality of rats with reducing the ratio of myocardial infarct to area at risk.
