The targeted inhibition of 11β-HSD1 leads to reduced blood glucose levels in hyperglycemic mice, highlighting the therapeutic potential of selective 11β-HSD1 inhibitors for addressing diseases with significant unmet medical needs, such as type 2 diabetes, obesity, and metabolic syndrome. BVT-14225 is notably effective in enzyme assays, achieving 90% inhibition at a concentration of 10 μM, and exhibits an IC50 of 52 nM against the human enzyme[2].
体外研究
The targeted inhibition of 11β-HSD1 leads to reduced blood glucose levels in hyperglycemic mice, highlighting the therapeutic potential of selective 11β-HSD1 inhibitors for addressing diseases with significant unmet medical needs, such as type 2 diabetes, obesity, and metabolic syndrome. BVT-14225 is notably effective in enzyme assays, achieving 90% inhibition at a concentration of 10 μM, and exhibits an IC50 of 52 nM against the human enzyme[2].
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