BVT 2733

BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC₅₀=96 nM) over the human enzyme (IC₅₀=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease^[1]. IC50 & Target:IC50: 96 nM (mouse 11β-HSD1)
IC50: 3341 nM (human 11β-HSD1)^[1] In Vitro: BVT 2733 (100 μM; 24 hours) co-treatment with PA (100 μM) reduces MCP-1 expression in fully differentiation adipocytes^[3].
BVT 2733 (50-100 μM; 24 hours) reduces the inflammation protein levels (MCP-1, IL-6) in medium?in J774.1 macrophages by Elisa^[3].
In Vivo: BVT-2733 (oral administration; 100 mg/kg; twice daily; 2 weeks) attenuates the arthritis severity and anti-CII level and decreases the levels of serum TNF-α, IL-1β, IL-6 and IL-17 in CIA mice^[2].
BVT 2733 (oral administration; 100 mg/kg; dosed (09.00 and 17.00 h); last 4 weeks) exhibits decreased body weight and enhanced glucose tolerance and insulin sensitivity when it compares to control mice. It also down-regulated the expression of inflammation-related genes including monocyte chemoattractant protein 1 (MCP-1), tumor necrosis factor alpha (TNF-α) and the number of infiltrated macrophages within the adipose tissue in vivo^[3].