JTT-654 is a potent and selective orally active inhibitor of 11beta-Hydroxysteroid dehydrogenase type 1 (11beta-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 11beta-HSD2 is greater than 30 µM, as this enzyme is responsible for the reverse reaction against human 11beta-HSD1. JTT-654 improves insulin resistance and non-obese type 2 diabetes by targeting 11beta-HSD1 in adipose tissue and the liver [1] [2].
Molekulargewicht:
530.58
CAS Nummer:
[916828-66-5]
Formel:
C28H33F3N4O3
Target-Kategorie:
Dehydrogenase
T86776
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