Search Result
Results for "
11 beta-hydroxysteroid dehydrogenase
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-14598
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Estrogen Receptor/ERR
Apoptosis
Autophagy
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Endocrinology
Cancer
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Diethylstilbestrol is a non-steroidal female hormone that has oral activity and can act on menopausal and postmenopausal disorders. Diethylstilbestrol can induce DNA oxidation and Apoptosis of spermatogonial stem cells. Diethylstilbestrol can induce thymocyte Autophagy Diethylstilbestrol is a 11β-hydroxysteroid dehydrogenase 2 (HSD11B2) inhibitor. .
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- HY-114464
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4-Androsten-11β-ol-3,17-dione
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Endogenous Metabolite
11β-HSD
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Endocrinology
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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 .
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- HY-124529
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11β-HSD
Endogenous Metabolite
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Metabolic Disease
Inflammation/Immunology
Cancer
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Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1, with an IC50 of 45.44 μM and a Ki of 35.8 μM against human 11β-HSD1, and an IC50 of 17.39 μM and a Ki of 10.31 μM against rat 11β-HSD1. Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4-mediated NF-κB pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human 11β-HSD1 and the steroid/NADPH-binding region of rat 11β-HSD1, but does not inhibit 11β-HSD2 or mouse 11β-HSD1. Lunularin can be used in research related to diet-induced obesity, renal cancer, colorectal cancer, inflammatory diseases and metabolic syndrome .
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- HY-18056
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11β-HSD
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Metabolic Disease
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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 .
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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-N2337
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11β-Hydroxyprogesterone
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11β-HSD
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Cardiovascular Disease
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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.
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- HY-114464S1
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4-Androsten-11β-ol-3,17-dione-d7
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Endogenous Metabolite
11β-HSD
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Others
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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
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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-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-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-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-W011243
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11β-HSD
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Cardiovascular Disease
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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.
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- HY-W741510
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21-Desoxycortisone; NSC 38722
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Endogenous Metabolite
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Cardiovascular Disease
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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-123800
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VTP-34072
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11β-HSD
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Neurological Disease
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BI 187004 (VTP-34072) is an 11β-hydroxysteroid dehydrogenase 1 inhibitor for use in diabetes research .
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- HY-111262
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11β-HSD
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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-14598R
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Reference Standards
Estrogen Receptor/ERR
Apoptosis
Autophagy
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Endocrinology
Cancer
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Diethylstilbestrol (Standard) is the analytical standard of Diethylstilbestrol. This product is intended for research and analytical applications. Diethylstilbestrol (Stilbestrol) is a non-steroidal female hormone that has oral activity and can act on menopausal and postmenopausal disorders. Diethylstilbestrol can induce DNA oxidation and Apoptosis of spermatogonial stem cells. Diethylstilbestrol can induce thymocyte Autophagy Diethylstilbestrol is a 11β-hydroxysteroid dehydrogenase 2 (HSD11B2) inhibitor. .
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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-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-120496
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ASP3662
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11β-HSD
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Neurological Disease
Metabolic Disease
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Clofutriben (ASP3662) is a selective, orally active and brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with Ki 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 .
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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-W754031
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11β-HSD
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Others
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11-Dehydrodexamethasone, Dexamethasone (HY-14648) derivative, is a substrate for 11β-hydroxysteroid dehydrogenase (11β-HSD) 1/2. 11-Dehydrodexamethasone undergoes conversion to Dexamethasone via reductive activity of 11β-HSD .
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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-114464S
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4-Androsten-11β-ol-3,17-dione-d4
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Isotope-Labeled Compounds
Endogenous Metabolite
11β-HSD
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Endocrinology
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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 .
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- HY-117428
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11β-HSD
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Metabolic Disease
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INU-101 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase (11β-HSD) type 1 inhibitor. INU-101 has highly potent inhibitory activity in mouse, monkey and human 11β-HSD1, derived from liver microsomes. INU-101 can enhance insulin sensitivity and lower the fasting blood glucose level. INU-101 can be used for the research of metabolic disease, such as diabetes .
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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-B1588S
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Amyloid-β
HIV
11β-HSD
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Infection
Neurological Disease
Inflammation/Immunology
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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 . Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease . Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD . Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop .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 .
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- HY-E71182
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Biochemical Assay Reagents
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Others
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11β-Hydroxysteroid dehydrogenase (EC 1.1.1.146) catalyze the conversion of inert 11 keto-products (cortisone) to active cortisol, or vice versa, thus regulating the access of glucocorticoids to the steroid receptors.
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- HY-120643A
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11β-HSD
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Metabolic Disease
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BMS-823778 was developed as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 to inhibit type 2 diabetes .
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- HY-18057
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AMG-311
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11β-HSD
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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-N2337R
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11β-Hydroxyprogesterone (Standard)
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Reference Standards
11β-HSD
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Cardiovascular Disease
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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.
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- HY-117609
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11β-HSD
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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-167696
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11β-HSD
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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-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-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-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-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-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-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-18056R
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11β-HSD
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Metabolic Disease
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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 .
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- HY-155535
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17β-HSD
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Neurological Disease
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17β-HSD10-IN-2 (compound 11) is a benzothiazolylurea-based inhibitor,targeting to 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10),a multifunctional mitochondrial enzyme. 17β-HSD10-IN-2 don't lead to mitochondrial off-targets and cytotoxic or neurotoxic effects. 17β-HSD10 inhibitors can be used for research in Alzheimer's disease (AD) and hormone-dependent cancer .
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- HY-105286A
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11β-HSD
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Metabolic Disease
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BI-135585 hydrate is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC50 of 13 nM. BI-135585 hydrate exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 hydrate can be used for type 2 diabetes research .
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- HY-180915
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17β-HSD
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Cancer
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Dehydrofalcarinol is a polyacetylene compound found in Desmanthodium guatemalense with anticancer activity. Dehydrofalcarinol shows anticancer activity depending on 17β-hydroxysteroid dehydrogenase (17β-HSD) type 11. Dehydrofalcarinol can be used for the research of triple-negative breast cancer .
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- HY-125421
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11β-HSD
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Metabolic Disease
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11β-HSD1-IN-26 (Compound 9f) is a type 1 11β-hydroxysteroid dehydrogenase (11β-HSD-1) inhibitor, with an IC50 of 1.6 nM against the human form and 241 nM against the murine form. 11β-HSD1-IN-26 exhibits inhibitory activity against CYP1C19, with an IC50 of 2 μM. 11β-HSD1-IN-26 can be used for research on metabolic syndrome .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-114464
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4-Androsten-11β-ol-3,17-dione
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Endogenous metabolite
Disease Research Fields
Endocrinology
Steroids
Source Classification
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Endogenous Metabolite
11β-HSD
|
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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 .
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- HY-124529
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Structural Classification
Human Gut Microbiota Metabolites
other families
Conocephalum conicum (L.) Dumort.
Phenols
Polyphenols
Plants
Endogenous metabolite
Source Classification
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11β-HSD
Endogenous Metabolite
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Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1, with an IC50 of 45.44 μM and a Ki of 35.8 μM against human 11β-HSD1, and an IC50 of 17.39 μM and a Ki of 10.31 μM against rat 11β-HSD1. Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4-mediated NF-κB pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human 11β-HSD1 and the steroid/NADPH-binding region of rat 11β-HSD1, but does not inhibit 11β-HSD2 or mouse 11β-HSD1. Lunularin can be used in research related to diet-induced obesity, renal cancer, colorectal cancer, inflammatory diseases and metabolic syndrome .
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- HY-N2337
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- HY-N2337R
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- HY-155535
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Optimized version of product available:
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-114464S1
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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
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- HY-114464S
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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 .
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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 . Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease . Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD . Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop .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 .
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