Search Result
Results for "
11beta-HSD
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-W106057
-
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11β-HSD
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Neurological Disease
Metabolic Disease
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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 .
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- HY-W129359
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11β-HSD
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Neurological Disease
Metabolic Disease
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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 .
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- HY-151627
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- HY-W324243
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11β-HSD
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Metabolic Disease
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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 .
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- HY-14156
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11β-HSD
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Metabolic Disease
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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 .
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- HY-123090
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11β-HSD
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Metabolic Disease
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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 .
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- HY-145381
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11β-HSD
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Metabolic Disease
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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 .
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- HY-157161
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11β-HSD
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Cancer
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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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- HY-W324220
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11β-HSD
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Metabolic Disease
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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 .
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- HY-U00325
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11β-HSD
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Neurological Disease
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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.
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- HY-162026
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11β-HSD
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Metabolic Disease
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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 .
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- HY-160618
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11β-HSD
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Metabolic Disease
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11β-HSD2-IN-2 (compound 3) is a selective inhibitor for 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) with an IC50 of 300 nM .
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- HY-167696
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Others
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Neurological Disease
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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.
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- HY-161449
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11β-HSD
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Metabolic Disease
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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 .
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- HY-120643
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11β-HSD
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Metabolic Disease
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BMS-823778 hydrochloride is a potent, selective and orally active 11β-HSD1 inhibitor with an IC50 of 2.3 nM against human 11β-HSD1 .
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- HY-18173
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11β-HSD
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Metabolic Disease
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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 .
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- HY-112290
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11β-HSD
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Metabolic Disease
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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 .
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- HY-150701
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Glucocorticoid Receptor
Mineralocorticoid Receptor
11β-HSD
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Metabolic Disease
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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 .
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- HY-W588255
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- HY-107124
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11β-HSD
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Metabolic Disease
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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 .
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- HY-122028
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11β-HSD
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Metabolic Disease
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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 .
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- HY-18055
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11β-HSD
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Metabolic Disease
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BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 52 nM.
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- HY-18053
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11β-HSD
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Metabolic Disease
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AZD 4017 is a potent, selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) inhibitor, with an IC50 of 7 nM.
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- HY-129630
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Endogenous Metabolite
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Metabolic Disease
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Tetrahydrocortisol is cortisol metabolite. The urinary Tetrahydrocortisol/Tetrahydrocortisone ratio decreases with increasing 11β-hydroxysteroid dehydrogenase (11β-HSD) activity .
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- HY-18057
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AMG-311
|
11β-HSD
|
Metabolic Disease
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BVT-3498 (AMG-311) is an inhibitor for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) .
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- HY-111262
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11β-HSD
|
Neurological Disease
Metabolic Disease
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ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (Ki 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) .
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- HY-14393
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Emodin
Maximum Cited Publications
21 Publications Verification
Frangula emodin
|
SARS-CoV
Casein Kinase
Autophagy
11β-HSD
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Cancer
|
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 .
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- HY-101930
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11β-HSD
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Metabolic Disease
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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 .
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- HY-148454
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- HY-117609
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11β-HSD
|
Neurological Disease
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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 .
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- HY-129630S
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Endogenous Metabolite
|
Metabolic Disease
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Tetrahydrocortisol-d5 is the deuterium labeled Tetrahydrocortisol. Tetrahydrocortisol is cortisol metabolite. The urinary Tetrahydrocortisol/Tetrahydrocortisone ratio decreases with increasing 11β-hydroxysteroid dehydrogenase (11β-HSD) activity[1][2].
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- HY-14393S
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Frangula emodin-d4
|
Isotope-Labeled Compounds
SARS-CoV
Casein Kinase
Autophagy
11β-HSD
|
Cancer
|
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].
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- HY-14393R
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Frangula emodin (Standard)
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SARS-CoV
Casein Kinase
Autophagy
11β-HSD
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Cancer
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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 .
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- HY-19325
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11β-HSD
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Metabolic Disease
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SKI2852 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50s of 1.6 nM and 2.9 nM against mHSD1 and hHSD1, respectively .
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- HY-112290A
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11β-HSD
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Cardiovascular Disease
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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 .
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- HY-101930B
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11β-HSD
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Metabolic Disease
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(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 .
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- HY-10555
-
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11β-HSD
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Metabolic Disease
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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 .
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- HY-105286
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11β-HSD
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Metabolic Disease
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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 .
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- HY-18054
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11β-HSD
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Inflammation/Immunology
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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 .
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- HY-101930A
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11β-HSD
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Metabolic Disease
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(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 .
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- HY-B1367
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Gap Junction Protein
Orthopoxvirus
11β-HSD
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Infection
Inflammation/Immunology
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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.
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- HY-W741510
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21-Desoxycortisone; NSC 38722
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Endogenous Metabolite
|
Cardiovascular Disease
|
21-Deoxy Cortisone (21-Desoxycortisone; NSC 38722) is a corticosteroid metabolite of 11-ketoprogesterone. It is formed from 11-ketoprogesterone by the cytochrome P450 (CYP) isozyme CYP17A1, but can also be produced by oxidation of 21-deoxycortisone (HY-113405) by 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2). Congenital adrenal hyperplasia is an inborn error of metabolism characterized by a deficiency of 21-hydroxylase, and 21-Deoxy Cortisone levels are elevated in patients with congenital adrenal hyperplasia.
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- HY-148682
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Glycyrrhetic acid 3-O-hydrogen sulfate
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OAT
11β-HSD
Drug Metabolite
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Metabolic Disease
Inflammation/Immunology
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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 .
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- HY-P5189A
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Endogenous Metabolite
Cholinesterase (ChE)
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Others
|
His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA, is a growth hormone releasing peptide, as well as a metabolite of GHRP-1. GHRP-1, or Ala-His-D-beta Nal-Ala-Trp-D-Phe-Lys-NH2, has the effect of promoting the release of growth hormone (GH). GHRP-1 increases GH release and increases [Ca2+]i levels in static monolayer cells of rat pituitary gland, but does not affect cAMP levels .
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- HY-B1588S
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Amyloid-β
HIV
11β-HSD
|
Infection
Neurological Disease
Inflammation/Immunology
|
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].
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P4285
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Peptides
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Others
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β-Aspartylalanine is a substrate for β-aspartyl peptidase and used to measure β-aspartyl peptidase activity in fecal supernatants .
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- HY-P5189A
-
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Endogenous Metabolite
Cholinesterase (ChE)
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Others
|
His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA, is a growth hormone releasing peptide, as well as a metabolite of GHRP-1. GHRP-1, or Ala-His-D-beta Nal-Ala-Trp-D-Phe-Lys-NH2, has the effect of promoting the release of growth hormone (GH). GHRP-1 increases GH release and increases [Ca2+]i levels in static monolayer cells of rat pituitary gland, but does not affect cAMP levels .
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Optimized version of product available:
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Product Name |
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- HY-129630S
-
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Tetrahydrocortisol-d5 is the deuterium labeled Tetrahydrocortisol. Tetrahydrocortisol is cortisol metabolite. The urinary Tetrahydrocortisol/Tetrahydrocortisone ratio decreases with increasing 11β-hydroxysteroid dehydrogenase (11β-HSD) activity[1][2].
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- HY-14393S
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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].
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- HY-B1588S
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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].
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