Search Result
Results for "
11β-HSD
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-14393
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Frangula emodin
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SARS-CoV
Casein Kinase
Autophagy
11β-HSD
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Cancer
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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-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-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-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-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-N0660
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Apoptosis
PARP
Caspase
AMPK
Autophagy
VEGFR
Keap1-Nrf2
STING
11β-HSD
Ferroptosis
PI3K
Akt
p38 MAPK
ERK
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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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, PM2.5-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 .
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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-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-N6711
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HIV Integrase
Bacterial
Antibiotic
Reactive Oxygen Species (ROS)
STAT
AMPK
11β-HSD
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Infection
Metabolic Disease
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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 [11].
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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-148454
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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-151627
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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-14393R
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Frangula emodin (Standard)
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Reference Standards
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-W588255
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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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-14393S
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Frangula emodin-d4
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Isotope-Labeled Compounds
SARS-CoV
Casein Kinase
Autophagy
11β-HSD
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Cancer
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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 . 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-112290
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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-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-169739
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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-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-180549
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11β-HSD
AMPK
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Metabolic Disease
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11β-HSD1-IN-25 is a selective and orally active 11β-HSD1 inhibitor. 11β-HSD1-IN-25 effectively reduces glucocorticoid levels in vitro and serum, and diminishes lipid accumulation in both vitro and vivo. 11β-HSD1-IN-25 modulates lipid metabolism through dual mechanisms: inhibition of 11β-HSD1 and activation of the AMP-activated protein kinase (AMPK) signaling pathway. 11β-HSD1-IN-25 can be used for obesity and related metabolic disorders research .
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- HY-18054A
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11β-HSD
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Inflammation/Immunology
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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 .
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- HY-178691
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11β-HSD
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Metabolic Disease
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11β-HSD1-IN-24 (Compound 10l) is a potent and selective 11β-HSD1 inhibitor with an IC50 of 0.5 nM. 11β-HSD1-IN-24 can effectively block the conversion of inactive Cortisone (HY-17461) to active Cortisol (HY-N0583). 11β-HSD1-IN-24 can be used for the research of metabolic disease, such as type 2 diabetes .
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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-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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- HY-179602
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PROTACs
11β-HSD
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Metabolic Disease
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PROTAC 11β-HSD1 Degrader 1 is a highly efficient PROTAC targeting 11β-HSD1 (Hydroxysteroid 11-beta dehydrogenase 1). PROTAC 11β-HSD1 Degrader 1 demonstrates ubiquitin-proteasome-dependent degradation of 11β-HSD1. PROTAC 11β-HSD1 Degrader 1 can be used for the study of type 2 diabetes mellitus (T2DM) .
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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-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-W342082
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11KP4
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11β-HSD
Cytochrome P450
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Cancer
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11-Ketoprogesterone (11KP4) is the substrate for CYP17A1 and 11β-HSD2 that could be metabolized to 21-deoxycortisone (21dE) and 21-deoxycortisol (21dF) with glucocorticoid activity .
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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-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-18054R
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11β-HSD
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Inflammation/Immunology
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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 .
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- HY-W755367
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11β-HSD
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Others
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Methyl glycyrrhetinate, a 18b-glycyrrhetinic acid analogue, is a dual inhibitor of 11β-HSD1 and 11β-HSD2 .
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- HY-183905
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11β-HSD
Glucocorticoid Receptor
Reactive Oxygen Species (ROS)
Keap1-Nrf2
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Neurological Disease
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KR-67607 is a selective 11β-HSD1 inhibitor, with an IC50 value of 4.8 nM against h11β-HSD1 and 7.1 nM against mouse 11β-HSD1. KR-67607 inhibits stress-induced Glucocorticoid receptor nuclear translocation, reduces cortisol levels, suppresses the expression of ROS and proinflammatory cytokines, and enhances Nrf-2-mediated antioxidant gene transcription. KR-67607 maintains trabecular meshwork structure and reverses elevated intraocular pressure. KR-67607 improves ocular antioxidant activity and mucus secretion, reverses ocular surface damage, and prevents ischemia-reperfusion induced ocular injury. KR-67607 can be used in research related to glaucoma and dry eye disease .
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- HY-179603
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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-N0660R
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Reference Standards
ERK
p38 MAPK
Akt
PI3K
11β-HSD
STING
VEGFR
Ferroptosis
Autophagy
Apoptosis
Keap1-Nrf2
Caspase
PARP
AMPK
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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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, PM2.5-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.
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Product Name |
Category |
Target |
Chemical Structure |
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- HY-14393
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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-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-N0660
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Cardiovascular Disease
Triterpenes
Structural Classification
other families
Classification of Application Fields
Terpenoids
Plants
Disease Research Fields
Source Classification
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Apoptosis
PARP
Caspase
AMPK
Autophagy
VEGFR
Keap1-Nrf2
STING
11β-HSD
Ferroptosis
PI3K
Akt
p38 MAPK
ERK
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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, PM2.5-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 .
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- HY-N6711
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- HY-14393R
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- HY-N0660R
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Triterpenes
Structural Classification
other families
Terpenoids
Plants
Source Classification
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Reference Standards
ERK
p38 MAPK
Akt
PI3K
11β-HSD
STING
VEGFR
Ferroptosis
Autophagy
Apoptosis
Keap1-Nrf2
Caspase
PARP
AMPK
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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, PM2.5-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.
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* This product has been "discontinued".
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-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 . 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-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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Reactivity |
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Yes
No
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| Size |
* This product has been "discontinued".
Optimized version of product available:
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| Cat. No. |
Product Name |
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Classification |
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- HY-179603
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Azide
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E3 Ligase Ligand-linker Conjugate 220 is an E3 ligase ligand-linker conjugate, can be used for synthesis of PROTAC 11β-HSD1 Degrader 1 (HY-179602) .
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