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.”

11β-HSD Related Products (60)
Antibodies (1)

By Effects:	Control (1) Inhibitors (52) Substrate (1) Inducer (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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.

HY-14393R

Emodin (Standard)	Inhibitor
Emodin (Standard) is the analytical standard of Emodin. This product is intended for research and analytical applications. 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. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. 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.

HY-120643

BMS-823778 hydrochloride	Inhibitor
BMS-823778 hydrochloride is a potent, selective and orally active 11β-HSD1 inhibitor with an IC₅₀ of 2.3 nM against human 11β-HSD1.

HY-117609

UE2343	Inhibitor
UE2343 is an orally available, brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. UE2343 is being investigated for the treatment of Alzheimer's disease.

HY-169739

DG 381B	Inhibitor
DG 381B (compound 62) is a 11β-HSD1 and 11β-HSD2inhibitor.

HY-112290A

MK-0736 hydrochloride	Inhibitor
MK-0736 hydrochloride is a potent and selective 11β-HSD-1 inhibitor with hypertension-reducing activity. MK-0736 hydrochloride can be used in studies related to metabolic syndrome. MK-0736 hydrochloride has demonstrated good antihypertensive effects and safety in clinical studies.

HY-W106057

11β-HSD1-IN-7		99.73%
11β-HSD1-IN-7 (compound c10a) is a 11β HSD1 inhibitor with an IC₅₀ value of 1.9 μM for human 11β HSD1. 11β-HSD1-IN-7 can be used for the research of diabetes and cognitive decline.

HY-101930B

(R)-BMS-816336	Inhibitor
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC₅₀s of 14.5 nM, 50.3 nM and 16 nM, respectively .

HY-120496

Clofutriben	Inhibitor
Clofutriben (ASP3662) is a 11β-hydroxysteroid dehydrogenase type 1 inhibitor.

HY-105286

BI-135585	Inhibitor
BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC₅₀ of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research.

HY-18056R

PF-915275 (Standard)	Inhibitor
PF-915275 (Standard) is the analytical standard of PF-915275. This product is intended for research and analytical applications. PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively.

HY-167696

11β-HSD1-IN-16	Inhibitor
11β-HSD1-IN-16 is an inhibitor of the 11β-hydroxysteroid dehydrogenase HSD11B1, demonstrating an IC of 0.34 μM, making it a valuable tool for research on neuropathic pain, inflammatory pain, and occipital neuralgia.

HY-14156

11β-HSD1-IN-15	Inhibitor
11β-HSD1-IN-15 is an inhibitor of 11β-hydroxysteroid dehydrogenase type I (11β-HSD1). 11β-HSD1-IN-15 blocks the conversion of corticosterone to cortisol by binding to the active site of the 11β-HSD1 enzyme. 11β-HSD1-IN-15 can be used to investigate the role of 11β-HSD1 enzymes IN the development of metabolic syndrome, obesity, cognitive decline and type 2 diabetes.

HY-18054R

BVT 2733 (Standard)	Inhibitor
BVT 2733 (Standard) is the analytical standard of BVT 2733. This product is intended for research and analytical applications. BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease.

HY-162026

11β-HSD1-IN-14	Inhibitor
11β-HSD1-IN-14 (Compound 17) is a selective inhibitor for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1), with IC₅₀ of 74 nM for human HSD1, and 603 nM for HSD1 expressed HEK293 cell.

HY-161449

JTT-654	Inhibitor
JTT-654 is an orally active, potent and selective11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. The IC₅₀ of JTT-654 for 11β-HSD1 is 4.65, 0.97, and 0.74 nM in human, rat, and mouse recombinant enzymes, respectively. JTT-654 showed competitive inhibition against human recombinant enzyme. The IC₅₀ value for human 11β-HSD2 is > 30 μM (human 11β-HSD2 is responsible for the reverse reaction against human 11β-HSD1). JTT-654 ameliorates insulin resistance and non-obese type 2 diabetes by inhibiting adipose tissue and liver 11β-HSD1.

HY-N2337R

11beta-Hydroxyprogesterone (Standard)	Inhibitor
11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.

HY-18054A

BVT-2733 hydrochloride	Inhibitor
BVT-2733 hydrochloride is a potent, selective and orally active nonsteroidal 11β-HSD1 inhibitor. BVT-2733 hydrochloride is more potent against mouse 11β-HSD1 enzyme (IC₅₀=96 nM) than against human 11β-HSD1 enzyme (IC₅₀=3341 nM). BVT-2733 hydrochloride has the potential to be used in the study of arthritis and obesity-related diseases.

HY-18057

BVT-3498	Inhibitor
BVT-3498 (AMG-311) is an inhibitor for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

HY-157161

11β-HSD2-IN-1	Inhibitor
11β-HSD2-IN-1 (compound CDSN) is a potent inhibitor of 11β-HSD2, inhibiting the metabolism of Cholestane-3β,5α,6β-triol (CT) in cells by 11β-HSD2 into the tumor promoter, carcinosterone. 11β-HSD2-IN-1 inhibits testosterone biosynthesis, thereby inhibiting MCF-7 cell proliferation. 11β-HSD2-IN-1 has immune activity and antiviral infection effects.

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11β-HSD

11β-HSD Related Products (60)

Antibodies (1)

11β-HSD Related Products (60):