JTT-654

JTT-654 is a potent and selective orally active inhibitor of 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1). It exhibits IC50 values of 4.65, 0.97, and 0.74 nM for human, rat, and mouse recombinant enzymes, respectively, and demonstrates competitive inhibition against the human recombinant enzyme. The IC50 value for human 11β-HSD2 is greater than 30 μM, as this enzyme is responsible for the reverse reaction against human 11β-HSD1. JTT-654 improves insulin resistance and non-obese type 2 diabetes by targeting 11β-HSD1 in adipose tissue and the liver [1] [2].