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 (75)
Antibodies (1)

By Effects:	Inhibitors (64) Degrader (1) Control (1) Substrates (2) Inducer (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-18055

BVT-14225	Inhibitor	98.23%
BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC₅₀ of 52 nM.

HY-148454

Necroptosis-IN-3	Inhibitor	99.53%
Necroptosis-IN-3 (Compound 69) is a necroptosis inhibitor that inhibits TNF-α induced necroptosis. Necroptosis-IN-3 (Compound STX1638) also inhibits 11β-HSD1.

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.

HY-W588255

Tetrahydro-11-dehydrocorticosterone	Inhibitor	99.79%
Tetrahydro-11-dehydrocorticosterone is a 11β-HSD inhibitor.

HY-123800

BI 187004		98.13%
BI 187004 (VTP-34072) is an 11β-hydroxysteroid dehydrogenase 1 inhibitor for use in diabetes research.

HY-107124

BMS-770767	Inhibitor	99.90%
BMS-770767 is an 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor in type 2 diabetes. 11β-HSD1 is an important enzyme that is widely expressed in liver, adipose tissue and other tissues and plays an important role in metabolic diseases such as diabetes and obesity.

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-101930

BMS-816336	Inhibitor	99.86%
BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC₅₀ of 3.0 nM.

HY-101930A

(Rac)-BMS-816336	Inhibitor	99.91%
(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.

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.

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.

HY-120496

Clofutriben	Inhibitor
Clofutriben (ASP3662) is a selective, orally active and brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with K_i values of 5.3 nM (human), 2.6 nM (mouse), and 23 nM (rat). Clofutriben inhibits conversion of inactive glucocorticoids to active glucocorticoids, reducing intracellular glucocorticoid exposure. Clofutriben ameliorates neuropathic pain, and restores muscle pressure thresholds in rodent models, while lacking effects in inflammatory pain.

HY-111262

ABT-384	Inhibitor	99.85%
ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (K_i 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD).

HY-167696

11β-HSD1-IN-16	Inhibitor	99.03%
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-U00325

11β-HSD1-IN-1	Inhibitor	99.85%
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.

HY-114464S

11-Beta-hydroxyandrostenedione-d₄	Inhibitor	98.3%
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.

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. 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-148682R

18β-Glycyrrhetyl-3-O-sulfate (Standard)	Inhibitor
(Z)-Methyl icos-11-enoate (Standard) is the analytical standard of (Z)-Methyl icos-11-enoate. This product is intended for research and analytical applications. (Z)-Methyl icos-11-enoate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.

HY-N0660R

Jujuboside B (Standard)	Inhibitor
Jujuboside B (Standard) is the analytical standard of Jujuboside B. This product is intended for research and analytical applications. Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway. Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM_2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes.

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.

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11β-HSD

11β-HSD Related Products (75)

Antibodies (1)

11β-HSD Related Products (75):