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 (53)
Antibodies (1)

By Effects:	Control (1) Inhibitors (47)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-14393

Emodin	Inhibitor	99.25%
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-B1367

Carbenoxolone disodium	Inhibitor	99.94%
Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation. Carbenoxolone disodium inhibits Vaccinia virus replication.

HY-18053

AZD 4017	Inhibitor	98.89%
AZD 4017 is a potent, selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) inhibitor, with an IC₅₀ of 7 nM.

HY-N2337

11beta-Hydroxyprogesterone	Inhibitor	99.91%
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-18054

BVT 2733	Inhibitor	99.72%
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-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.

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-150701

INCB13739	Inhibitor	99.79%
INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC₅₀ values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research.

HY-114464S1

11-Beta-hydroxyandrostenedione-d₇	Inhibitor	≥99.0%
11-Beta-hydroxyandrostenedione-d₇ 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]

HY-114464

11-Beta-hydroxyandrostenedione	Inhibitor	99.74%
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. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism.

HY-160618

11β-HSD2-IN-2	Inhibitor	99.96%
11β-HSD2-IN-2 (compound 3) is a selective inhibitor for 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) with an IC₅₀ of 300 nM.

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-W011243

11alpha-Hydroxyprogesterone	Control	99.09%
11alpha-Hydroxyprogesterone is the analogue of 11beta-Hydroxyprogesterone (HY-N2337), and can be used as an experimental control. 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-148454

Necroptosis-IN-3	Inhibitor	99.77%
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-N6711

Equisetin	Inhibitor	99.40%
Equisetin is an N-methylserine-derived acyl tetramic acid, quorum sensing inhibitor (QSI), herbicides and antibiotics. Equisetin specifically inhibits the anionic carriers of substrates in the inner mitochondrial membrane. Equisetin inhibits the activity of HIV-1 integrase, 11β-HSD1, and 2,4-dinitrophenol (Dnp)-stimulated ATPase (IC₅₀ = ~8 nmol per mg of protein). Equisetin exhibits growth inhibition of bacteria, anti-inflammatory, amelioration of lipid-associated disorders, and cytotoxic effects.

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-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-148682

18β-Glycyrrhetyl-3-O-sulfate	Inhibitor	98.01%
18β-Glycyrrhetyl-3-O-sulfate (Glycyrrhetic acid 3-O-(hydrogen sulfate)) is a potent type 2 11β-hydroxysteroid dehydrogenase (11β-HSD2) inhibitor with an IC₅₀ of 0.10 µM using rat kidney microsome. 18β-Glycyrrhetyl-3-O-sulfate is the major metabolite of Glycyrrhetinic acid (GA). 18β-Glycyrrhetyl-3-O-sulfate is the substrate of organic anion transporter (OAT) 1 and OAT3. 18β-Glycyrrhetyl-3-O-sulfate has anti-inflammatory effects and has the potential for pseudohyperaldosteronism research.

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.

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11β-HSD

11β-HSD Related Products (53)

Antibodies (1)

11β-HSD Related Products (53):