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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V73869 | 11β-HSD1-IN-10 | 849021-37-0 | 11β-HSD1-IN-10 (compound c3a) is a potent inhibitor of 11β-HSD1 (IC50=1.8 µM for humans). |
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V73867 | 11β-HSD1-IN-11 | 859721-81-6 | 11β-HSD1-IN-11 (Compound c1a) is a competitive 11β-HSD1 inhibitor (antagonist) with IC50 of 0.34 μM and 0.13 μM for rat and human 11β-HSD1, respectively. |
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V73868 | 11β-HSD1-IN-12 | 872506-67-7 | 11β-HSD1-IN-12 is an 11β-HSD1 inhibitor (Example 21 in the patent). |
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V87253 | 11β-HSD1-IN-14 | 946394-50-9 | 11β-HSD1-IN-14 (Compound 17) is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with IC50 of 74 nM (h 11β-HSD1) and 603 nM (HEK293 cells expressing HSD1). |
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V73866 | 11β-HSD1-IN-7 | 728-86-9 | 11β-HSD1-IN-7 (compound c10a) is an inhibitor (blocker/antagonist) of 11β-HSD1 with IC50 of 1.9 μM for human 11β-HSD1. |
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V73870 | 11β-HSD1-IN-8 | 386704-15-0 | 11β-HSD1-IN-8 (compound c6a) is an inhibitor (blocker/antagonist) of 11β-HSD1 with IC50 of 2.3 μM for human 11β-HSD1. |
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V73871 | 11β-HSD1-IN-9 | 88283-34-5 | 11β-HSD1-IN-9 (compound c4a) is a potent 11β-HSD1 inhibitor (antagonist) with IC50s of 0.48 and 1.3 µM for human and murine 11β-HSD1, respectively. |
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V77509 | 11β-HSD2-IN-1 | 11β-HSD2-IN-1 (compound CDSN) is a potent inhibitor of 11β-HSD2, inhibiting 11β-HSD2 from metabolizing cholestane-3β,5α,6β-triol (CT) in cells into the tumor promoter, carcinosterone. | |
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V87252 | 11β-HSD2-IN-2 | 1834601-37-4 | 11β-HSD2-IN-2 (compound 3) is a selective inhibitor of type 2 7β-hydroxysteroid dehydrogenase (17β-HSD2) with IC50 of 300 nM. |
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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. |
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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. |
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V17296 | BVT-14225 | 376638-65-2 | BVT-14225 is a selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor (antagonist) with IC50 of 52 nM. |
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V73865 | Clofutriben (ASP3662) | 1204178-50-6 | Clofutriben (ASP3662) is an 11β-hydroxysteroid dehydrogenase type 1 inhibitor. |
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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. |
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V87254 | JTT-654 | 916828-66-5 | JTT-654 is an orally active, selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. |
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V94232 | MK-0736 hydrochloride | 719274-77-8 | MK-0736 hydrochloride is a potent and selective 11β-HSD-1 inhibitor with antihypertensive activity. |
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V51047 | Necroptosis-IN-3 | 547698-18-0 | Necroptosis-IN-3 (Compound 69) is a necroptosis inhibitor that can suppress TNF-α-induced necroptosis. |
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V73864 | Tetrahydro-11-dehydrocorticosterone | 566-03-0 | Tetrahydro-11-dehydrocorticosterone is an 11β-HSD inhibitor. |
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V96711 | UE2343 | 1346013-80-6 | UE2343 is an oral, brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. |
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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. |
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