CLT-28643 is a potent and specific α5β1-Integrin inhibitor that prevents fibrosis in glaucoma filtration surgery (GFS), inhibits tumor growth and angiogenesis, suppresses fibrosis and inflammation in a bleomycin-induced lung fibrosis model, and improves insulin sensitivity and cardiac function in H9C2 cells from obese mice.

In H9C2 cardiomyocytes, CLT-28643 (3 hours) was used to assess its effect on insulin signaling under metabolic stress, CLT-28643 prevented high glucose and palmitate-induced insulin resistance by significantly increasing the phosphorylated Akt (Ser473) to total Akt ratio, indicating restored insulin sensitivity. [1]

In male C57BL/6 mice fed a high-fat-high-sucrose (HFHS) diet for 10 weeks, CLT-28643 (75 mg/kg; oral gavage; twice daily for 4 weeks) was administered to evaluate its cardiometabolic effect. CLT-28643 improved cardiac function by reversing the HFHS diet-induced elevation in heart rate, suggesting enhanced cardiovascular performance. [1]