2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. 11β-HSD

11β-HSD

11beta-HSD; 11β-hydroxysteroid dehydrogenases; 11 beta-hydroxysteroid dehydrogenase

Two isozymes of 11β-hydroxysteroid dehydrogenase (11β-HSD) catalyze interconversion of active cortisol and corticosterone with inert cortisone and 11-dehydrocorticosterone. 11β-HSD type 1 (11β-HSD1), a predominant reductase in most intact cells, catalyzes the regeneration of active glucocorticoids, thus amplifying cellular action. 11β-HSD1 is selectively elevated in adipose tissue in obesity where it contributes to metabolic complications. Similarly, 11β-HSD1 is elevated in the ageing brain where it exacerbates glucocorticoid-associated cognitive decline. Deficiency or selective inhibition of 11β-HSD1 improves multiple metabolic syndrome parameters in rodent models and human clinical trials and similarly improves cognitive function with ageing. 11β-HSD2 is a high-affinity dehydrogenase that inactivates glucocorticoids. In the distal nephron, 11β-HSD2 ensures that only aldosterone is an agonist at mineralocorticoid receptors (MR). 11β-HSD2 inhibition or genetic deficiency causes apparent mineralocorticoid excess and hypertension due to inappropriate glucocorticoid activation of renal MR. The placenta and fetus also highly express 11β-HSD2 which, by inactivating glucocorticoids, prevents premature maturation of fetal tissues and consequent developmental “programming.”

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-18055
    BVT-14225
    		Inhibitor 98.01%
    BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 52 nM.
    BVT-14225
  • HY-18173
    AZD8329
    		Inhibitor 99.68%
    AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3.
    AZD8329
  • HY-W588255
    Tetrahydro-11-dehydrocorticosterone
    		Inhibitor 99.79%
    Tetrahydro-11-dehydrocorticosterone is a 11β-HSD inhibitor.
    Tetrahydro-11-dehydrocorticosterone
  • HY-123800
    BI 187004
    		98.13%
    BI 187004 (VTP-34072) is an 11β-hydroxysteroid dehydrogenase 1 inhibitor for use in diabetes research.
    BI 187004
  • HY-122028
    HSD-016
    		Inhibitor 99.95%
    HSD-016 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50 values of 11, 1 and 8 nM against human, mouse and rat 11β-HSD1, respectively. HSD-016 can be used for type 2 diabetes research.
    HSD-016
  • HY-W129359
    11β-HSD1-IN-8
    11β-HSD1-IN-8 (compound c6a) is a 11β HSD1 inhibitor with an IC50 value of 2.3 μM for human 11β HSD1. 11β-HSD1-IN-8 can be used for the research of diabetes and cognitive decline.
    11β-HSD1-IN-8
  • HY-114464S
    11-Beta-hydroxyandrostenedione-d4
    		Inhibitor
    11-Beta-hydroxyandrostenedione-d4 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor[1][2].
    11-Beta-hydroxyandrostenedione-d<sub>4</sub>
  • HY-U00325
    11β-HSD1-IN-1
    		Inhibitor 99.80%
    11β-HSD1-IN-1 is an inhibitor of 11β-hydroxydehydrogenase 1 (11β-HSD1), with an IC50 of 52 nM, and used for the treatment of pain.
    11β-HSD1-IN-1
  • HY-14393S
    Emodin-d4
    		Inhibitor
    Emodin-d4 is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice[3].
    Emodin-d<sub>4</sub>
  • HY-118113
    BVT-116429
    		Inhibitor
    BVT-116429 is an 11βHSD1 inhibitor with the activity of increasing adiponectin concentration and improving glucose homeostasis in diabetic mice. BVT-116429 can increase plasma adiponectin levels in diabetic KKAy mice, reduce basal insulin levels, and reduce fasting blood glucose levels after 10 days of inhibition, similar to the effect of rosiglitazone.
    BVT-116429
  • HY-10555
    AMG-221
    		Inhibitor
    AMG-221 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with a Ki of 12.8 nM in vitro biochemical scintillation proximity assay (SPA) and an IC50 of 10.1 nM in cell-based assays. AMG-221 can be used for the research of type 2 diabetes.
    AMG-221
  • HY-101930A
    (Rac)-BMS-816336
    		Inhibitor
    (Rac)-BMS-816336 (Compound 6n) is a racemate of BMS-816336. (Rac)-BMS-816336 is a potent inhibitor of human and mouse 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 10 nM and 68 nM, respectively. (Rac)-BMS-816336 has good metabolic stability.
    (Rac)-BMS-816336
  • HY-W324243
    11β-HSD1-IN-9
    11β-HSD1-IN-9 (compound c4a) is a potent 11β-HSD1 inhibitor with IC50 values of 0.48 and 1.3 µM for human and murine 11β-HSD1, respectively. 11β-HSD1-IN-9 competitively interacts with rat 11β-HSD1. 11β-HSD1-IN-19 can be used in studies of obesity, hyperglycemia and cognitive impairment.
    11β-HSD1-IN-9
  • HY-123090
    11β-HSD1-IN-12
    		Inhibitor
    11β-HSD1-IN-12 is a 11β-HSD1 inhibitor (Example 21 in reference patent). 11β-HSD1 regenerates active glucocorticoids from inactive forms and is important in regulating intracellular glucocorticoid concentration. 11β-HSD1-IN-12 can be used in the research of obesity and metabolic syndrome.
    11β-HSD1-IN-12
  • HY-151627
    11β-HSD1-IN-11
    		Inhibitor
    11β-HSD1-IN-11 (Compound c1a) is a competitive 11β-HSD1 inhibitor with IC50s of 0.34 μM and 0.13 μM against rat and human 11β-HSD1, respectively.
    11β-HSD1-IN-11
  • HY-W324220
    11β-HSD1-IN-10
    11β-HSD1-IN-10 (compound c3a) is a potent 11β-HSD1 inhibitor (IC50=1.8 µM for human). 11β-HSD1-IN-10 can be used in studies of obesity, hyperglycemia and cognitive impairment.
    11β-HSD1-IN-10
  • HY-120643A
    BMS-823778
    		Inhibitor
    BMS-823778 was developed as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 to inhibit type 2 diabetes.
    BMS-823778
  • HY-B1588S
    Carbenoxolone-d4
    		Inhibitor
    Carbenoxolone-d4 is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties[3]. Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease[2]. Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD[1]. Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop[4].Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself[6].
    Carbenoxolone-d<sub>4</sub>
  • HY-112290
    MK-0736
    		Inhibitor
    MK-0736 is a 11β-HSD type 1 (11β-HSD1) inhibitor that reduces blood pressure. MK-0736 can be used for type 2 diabetes and metabolic syndrome research.
    MK-0736
  • HY-145381
    11β-HSD1-IN-6
    		Inhibitor
    11β-HSD1-IN-6 is a an 11β-HSD-1 inhibitor. The 11β hydroxysteroid dehydrogenase enzymes (11β-HSDs) mediate the interconversion of the glucocorticoid (GC) corticosterone or cortisol to an inactive form, 11-dehydrocorticosterone (11-DHC) or Cortisone, respectively.
    11β-HSD1-IN-6
Cat. No. Product Name / Synonyms Application Reactivity