BVT 2733 is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1.
ki: 1 μm using 11-dehydrocorticosterone as substratebvt 2733 is a novel, small molecule, non-steroidal, and selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-hsd1).11β-hsd1 has been reported to alter glucocorticoid hormone action in target tissues for insulin action and is suggested to play a key role in glucose homeostasis.
bvt 2733 was identified as a novel type 1 selective inhibitor of murine 11β-hsd1 (ki 1 μmol/l), which did not inhibit mouse 11β-hsd type 2 at a concentration as high as 200 μmol/l (corresponding to a ki >33 μmol/l). therefore, the selectivity of bvt 2733 for the 11β-hsd type 1 enzyme over the type 2 enzyme was estimated to be at least 30-fold based on the ki values [1].
in mice, bvt 2733 treatment could lower hepatic pepck and glucose-6-phosphatase mrna, serum insulin and blood glucose concentrations compared with vehicle treated mice. in contrast, hepatic 11beta-hydroxysteroid dehydrogenase type 1 mrna, liver function marker enzyme expression including alanine aminotransferase, aspartate aminotransferase and alkaline phosphatases, body weight as well as daily food intake were not changed by the treatment of bvt 2733 [1].
[1] alberts p,engblom l,edling n,forsgren m,klingstrm g,larsson c,rnquist-nii y,ohman b,abrahmsén l. selective inhibition of 11beta-hydroxysteroid dehydrogenase type 1 decreases blood glucose concentrations in hyperglycaemic mice. diabetologia.2002 nov;45(11):1528-32.
