BVT 14225

BVT 14225 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1; IC₅₀s = 52 and 284 nM for the human and mouse enzymes, respectively).¹ It is selective for human 11β-HSD1 over human 11β-HSD2 (IC₅₀ = >10,000 nM). It inhibits 11β-HSD1 by 55% in HEK293 cells expressing human HSD11B1, the gene encoding 11β-HSD1, when used at a concentration of 10 µM.² BVT 14225 (50 mg/kg) reduces blood glucose levels in a rat model of diabetes induced by streptozotocin (Item No. 13104) and nicotinamide (Item No. 11127).

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1. Barf, T., Vallgårda, J., Emond, R., et al. Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1. J. Med. Chem. 45(18), 3813-3815 (2002).

2. Navarrete-Vázquez, G., Morales-Vilchis, M.G., Estrada-Soto, S., et al. Synthesis of 2-{2-[(α/β-naphthalen-1-ylsulfonyl)amino]-1,3-thiazol-4-yl} acetamides with 11β-hydroxysteroid dehydrogenase inhibition and in combo antidiabetic activities. Eur. J. Med. Chem. 74, 179-186 (2014).