11β-HSD

11β-HSD

The interconversion of active cortisol and corticosterone with inert cortisone and 11-dehydrocorticosterone is catalyzed by two isozymes of 11-hydroxysteroid dehydrogenase (11-HSD). The regeneration of active glucocorticoids is catalyzed by 11-HSD type 1 (11-HSD1), a predominant reductase in the majority of intact cells, amplifying cellular action. In obesity, 11-HSD1 is primarily elevated in adipose tissue, where it plays a role in metabolic complications. Similar to this, 11-HSD1 is increased in the aging brain, where it exacerbates cognitive decline brought on by glucocorticoids.In rodent models and human clinical trials, 11-HSD1 deficiency or selective inhibition improves a number of metabolic syndrome parameters, and similar improvements in cognitive function with aging. A high-affinity dehydrogenase called 11-HSD2 renders glucocorticoids inactive. Only aldosterone is an agonist at mineralocorticoid receptors (MR) in the distal nephron due to 11-HSD2. Due to inappropriate glucocorticoid activation of renal MR, 11-HSD2 inhibition or genetic deficiency result in apparent mineralocorticoid excess and hypertension. Additionally, the fetus and placenta both highly express 11-HSD2, which, by inactivating glucocorticoids, prevents premature fetal tissue maturation and the ensuing "programming" of the fetus' development.

11β-HSD related products

Structure Cat No. Product Name CAS No. Product Description
V73869 11β-HSD1-IN-10 849021-37-0
V73867 11β-HSD1-IN-11 859721-81-6
V73868 11β-HSD1-IN-12 872506-67-7
V73866 11β-HSD1-IN-7 728-86-9
V73870 11β-HSD1-IN-8 386704-15-0
V73871 11β-HSD1-IN-9 88283-34-5
V77509 11β-HSD2-IN-1
V4237 AZD 4017 1024033-43-9 AZD4017,a nicotinic amide derived carboxylic acid, is a novel, potent, selective andeffective inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1(11β-HSD1) in human adipocytes with anIC50of 7 nM.
V3491 BMS-816336 1009583-20-3 BMS-816336 is a potent and orally bioactive inhibitor ofhuman 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzymewith anIC50of 3.0 nM.
V17296 BVT-14225 376638-65-2 BVT-14225 is a novel and potent 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor.
V11621 Carbenoxolone sodium 7421-40-1 Carbenoxolone sodium (Pyrogastrone;Biogastrone; Bioral; Duogastrone; Sanodin), an analogue of glycyrrhizin, isthe active metabolite of Glycyrrhizic acid and an inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD.
V73865 Clofutriben (ASP3662) 1204178-50-6
V41925 HSD-016 946396-92-5 HSD-016 (HSD016) is a novel 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor (IC50 = 11, 1 and 8 nM for human, mouse and rat 11β-HSD1, respectively) with the potential to be used for type 2 diabetes.
V51047 Necroptosis-IN-3 547698-18-0 Necroptosis inhibitor
V73864 Tetrahydro-11-dehydrocorticosterone 566-03-0
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