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Technology

ML278 and ML279 are two of the inhibitors of SR-BI that were discovered in a high throughput screen. These molecules work by increasing the binding of HDL to SR-BI while reversibly inhibiting the transfer of cholesterol. ML278 and ML279 were shown to inhibit SR-B1 both selectively and potently in the screen assay with IC50s of 6 and 17 nM, respectively. It is important to note that these lead compounds showed superior potency in the screen assays compared to the clinical SR-B1 inhibitor ITX-5061.