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HSD-1 inhibitor SPI-62

An orally bioavailable selective inhibitor of the enzyme 11beta-hydroxysteroid dehydrogenase type 1 (11b-HSD1; 11bHSD1; HSD11B1; HSD1; HSD-1), with potential protective activity for disorders of corticosteroid excess. Upon oral administration, HSD-1 inhibitor SPI-62 selectively binds to and inhibits the activity of HSD-1. This prevents the conversion of cortisone to the active hormone cortisol and thereby preventing the activation of the glucocorticoid receptors (GRs). By blocking cortisol production in metabolic tissues, SPI-62 may inhibit the adverse metabolic effects that are caused by exogenous administration of glucocorticoids or in disorders in which cortisol is secreted in excess. HSD-1 is highly expressed in metabolic tissues, such as liver, skeletal muscle, and adipose tissue. It plays a crucial role in regulating the production of cortisol to activate the GRs.
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Synonym:11beta-hydroxysteroid dehydrogenase type 1 inhibitor SPI-62
Code name:SPI 62
SPI-62
SPI62
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