BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 52 nM.
Selective inhibition of 11β-HSD1 decreases blood glucose concentrations in hyperglycaemic mice. Selective inhibitors of 11β-HSD1 have considerable potential as treatments for a number of diseases of great unmet medical need such as type 2 diabetes, obesity and metabolic syndrome, a multifactorial disorder. BVT-14225 shows high activity in the enzyme assay with 90% inhibition at 10 μM. It has an IC50 for 11β-HSD1 on a human enzyme assay of 52 nM[2].
[1]. Barf T, et al. Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1. J Med Chem. 2002 Aug 29;45(18):3813-5. [2]. Vicker N, et al. Novel non-steroidal inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1. J Steroid Biochem Mol Biol. 2007 May;104(3-5):123-9.