MMP-13-IN-1, with an IC50 value of 16 nM, is a potent and selective inhibitor of MMP-13, suitable for atherosclerosis research [1].

MMP13:16 nM

MMP-13-IN-1 (compound 5j) at a dosage of 2.5 mg/kg was administered intravenously 15 minutes before the radiotracer in ApoE −/− mice models. This study revealed that MMP-13-IN-1 exhibited low uptake by metabolic organs, minimal myocardial radioactivity retention, high renal clearance, and notable metabolic stability. It achieved the highest overall uptake and maximal colocalization with ORO positive areas. Results indicated a continuous decrease in blood radioactivity between 30 and 60 minutes, followed by stabilization. There was a significant reduction in liver uptake and relatively low radioactivity in other organs, except for the pancreas and spleen. The compound led to a 23% decrease in aortic plaque uptake, suggesting a degree of saturable binding.