11β-hsd2

11β-HSD2-IN-2 (compound 3) is a selective 17β-HSD2 (17β-hydroxysteroid dehydrogenase type 2) inhibitor with an IC50 of 300 nM, suitable for studying osteoporosis.

11β-HSD2-IN-1 (compound CDSN) serves as a potent inhibitor of 11β-HSD2, effectively hindering this enzyme from metabolizing Cholestane-3β,5α,6β-triol (CT) into carcinogenic androstenedione within cells. By inhibiting testosterone biosynthesis, 11β-HSD2-IN-1 suppresses the proliferation of MCF-7 cells. Additionally, this compound exhibits immunological activity and offers protection against viral infections.

AZD8329 is a selective and potent 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that inhibits 11β-HSD2, 17β-HSD1, 17β-HSD3, and can be used for the study of allergic reactions in humans.

Chenodeoxycholic acid (CDCA) is a bile acid that inhibits 11β-HSD2 with an IC50 value of 22 mM. Chenodeoxycholic acid acts as a detergent to dissolve fat for intestinal absorption and is reabsorbed by the small intestine. Chenodeoxycholic acid is used as a choledocholithiasis, choledocholithiasis and laxative, as well as to prevent or dissolve gallstones.

ASP3662, also known as SPI-62, is a potent, selective and CNS-penetrable inhibitor of 11β-HSD1. The effects of ASP3662 suggest that selective inhibition of 11β-HSD1 may be an attractive approach for the treatment of neuropathic and dysfunctional pain, as observed in fibromyalgia. ASP3662 inhibited human, mouse and rat 11β-HSD1 but not human 11β-HSD2, in vitro. ASP3662 inhibited in vitro conversion of glucocorticoid from its inactive to active form in extracts of rat brain and spinal cord.

18β-Glycyrrhetyl-3-O-sulfate (Glycyrrhetic acid 3-O-(hydrogen sulfate)), a major metabolite of Glycyrrhetinic acid (GA), is a potent inhibitor of type 2 11β-hydroxysteroid dehydrogenase (11β-HSD2) with an IC50 value of 0.10 µM in rat kidney microsome assays. This compound is a substrate for organic anion transporters (OAT) 1 and OAT3, exhibits anti-inflammatory properties, and holds potential for research into pseudohyperaldosteronism [1] [2].

JTT-654 is a potent and selective orally active inhibitor of 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1). It exhibits IC50 values of 4.65, 0.97, and 0.74 nM for human, rat, and mouse recombinant enzymes, respectively, and demonstrates competitive inhibition against the human recombinant enzyme. The IC50 value for human 11β-HSD2 is greater than 30 μM, as this enzyme is responsible for the reverse reaction against human 11β-HSD1. JTT-654 improves insulin resistance and non-obese type 2 diabetes by targeting 11β-HSD1 in adipose tissue and the liver [1] [2].

Chenodeoxycholic acid (Standard) is a reference standard for research and analysis in studies involving Chenodeoxycholic acid. Chenodeoxycholic acid (CDCA) is a bile acid that inhibits 11β-HSD2 with an IC50 value of 22 mM. Chenodeoxycholic acid acts as a detergent to dissolve fat for intestinal absorption and is reabsorbed by the small intestine. Chenodeoxycholic acid is used as a choledocholithiasis, choledocholithiasis and laxative, as well as to prevent or dissolve gallstones.

3-Hydroxylicochalcone A is a naturally occurring chalcone derivative. chalcone derivatives usually inhibit murine 11β-hydroxysteroid dehydrogenase 2 (11β-HSD2), e.g., Licochalcone A is the most potent of them all (IC50=15.6 μM).

21-Deoxy Cortisone (21-Desoxycortisone; NSC 38722) is a corticosteroid metabolite of 11-ketoprogesterone. It is generated from 11-ketoprogesterone by the cytochrome P450 (CYP) isoform CYP17A1, and can also be produced by oxidation via 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2) from 21-deoxycorticosterone. In patients with congenital adrenal hyperplasia, a metabolic disorder characterized by a deficiency of 21-hydroxylase, levels of 21-Deoxy Cortisone are elevated.