human 11β-hsd1

BI-135585 is an orally active, selective and potent inhibitor of human 11β-hydroxysteroid dehydrogenase-1 (HSD1) for the study of type 2 diabetes.

HSD-016 is an orally active, selective and potent type 1 11β-hydroxysteroid dehydrogenase (11β-HSD1) inhibitor with strong inhibitory effects on human, mouse and rat 11β-HSD1.HSD-016 can be used in the study of diabetes and metabolic syndrome.

BMS-823778 is a potent inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) for the study of type 2 diabetes.

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.

Emodin (Frangula emodin) is a naturally occurring anthraquinone present in the roots and barks of numerous plants; exerts antiproliferative effects in Y cells that are regulated by different signaling pathways.

BVT 2733 is a new, non-steroidal, isoform-specific inhibitor of 11β-HSD1.

BMS-823778 hydrochloride is a potent, selective, and orally active inhibitor of 11β-HSD1 (11β-Hydroxysteroid Dehydrogenase Type 1), with an IC50 (half maximal inhibitory concentration) of 2.3 nM against the human enzyme.

BVT-2733 hydrochloride is a potent, selective, and orally active non-steroidal 11β-HSD1 inhibitor. It exhibits stronger inhibition on mouse 11β-HSD1 enzyme (IC50=96 nM) compared to the human 11β-HSD1 enzyme (IC50=3341 nM). BVT-2733 hydrochloride shows potential for research in arthritis and obesity-related diseases.

ABT-384 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1.

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].

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.

(Rac)-BMS-816336 (Compound 6n), a racemate of BMS-816336, is a potent inhibitor of human and mouse 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with IC50 values of 10 nM and 68 nM, respectively, and demonstrates good metabolic stability [1].

11β-HSD1-IN-9 is a potent inhibitor of 11β-HSD1, displaying IC50 values of 0.48 µM for human and 1.3 µM for murine variants, respectively. It exhibits competitive interaction with rat 11β-HSD1. This compound holds potential utility in research focused on obesity, hyperglycemia, and cognitive impairment.