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11β-HSD1

" in MedChemExpress (MCE) Product Catalog:

56

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-14393
    Emodin
    35+ Cited Publications

    Frangula emodin

    		 SARS-CoV Casein Kinase Autophagy 11β-HSD 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 .
    Emodin
  • HY-124529
    Lunularin

    		11β-HSD Endogenous Metabolite Metabolic Disease Inflammation/Immunology Cancer
    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 .
    Lunularin
  • HY-18054
    BVT 2733
    4 Publications Verification

    		 11β-HSD Inflammation/Immunology
    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 .
    BVT 2733
  • HY-18056
    PF-915275

    		11β-HSD Metabolic Disease
    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 .
    PF-915275
  • HY-18055
    BVT-14225
    1 Publications Verification

    		 11β-HSD Metabolic Disease
    BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 52 nM.
    BVT-14225
  • HY-18053
    AZD 4017

    		11β-HSD Metabolic Disease
    AZD 4017 is a potent, selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) inhibitor, with an IC50 of 7 nM.
    AZD 4017
  • HY-N6711
    Equisetin

    		HIV Integrase Bacterial Antibiotic Reactive Oxygen Species (ROS) STAT AMPK 11β-HSD Infection Metabolic Disease
    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 .
    Equisetin
  • HY-148454
    Necroptosis-IN-3

    		Necroptosis 11β-HSD Inflammation/Immunology Cancer
    Necroptosis-IN-3 (Compound 69) is a necroptosis inhibitor that inhibits TNF-α induced necroptosis . Necroptosis-IN-3 (Compound STX1638) also inhibits 11β-HSD1 .
    Necroptosis-IN-3
  • HY-150701
    INCB13739

    		Glucocorticoid Receptor Mineralocorticoid Receptor 11β-HSD Metabolic Disease
    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 .
    INCB13739
  • HY-18173
    AZD8329

    		11β-HSD Metabolic Disease
    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 .
    AZD8329
  • HY-151627
    11β-HSD1-IN-11

    		11β-HSD Neurological Disease Metabolic Disease
    11β-HSD1-IN-11 (Compound c1a) is a competitive 11β-HSD1 inhibitor with IC50s of 0.34 μM and 0.13 μM against rat and human 11β-HSD1, respectively .
    11β-HSD1-IN-11
  • HY-14393R
    Emodin (Standard)
    35+ Cited Publications

    Frangula emodin (Standard)

    		 Reference Standards SARS-CoV Casein Kinase Autophagy 11β-HSD Cancer
    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 .
    Emodin (Standard)
  • HY-19325
    SKI2852

    		11β-HSD Metabolic Disease
    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 .
    SKI2852
  • HY-W106057
    11β-HSD1-IN-7

    		11β-HSD Neurological Disease Metabolic Disease
    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 .
    11β-HSD1-IN-7
  • HY-U00325
    11β-HSD1-IN-1

    		11β-HSD Neurological Disease
    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.
    11β-HSD1-IN-1
  • HY-111262
    ABT-384

    		11β-HSD Neurological Disease Metabolic Disease
    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) .
    ABT-384
  • HY-W129359
    11β-HSD1-IN-8

    		11β-HSD Neurological Disease Metabolic Disease
    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 .
    11β-HSD1-IN-8
  • HY-105286
    BI-135585

    		11β-HSD Metabolic Disease
    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 .
    BI-135585
  • HY-101930A
    (Rac)-BMS-816336

    		11β-HSD Metabolic Disease
    (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 .
    (Rac)-BMS-816336
  • HY-179602
    PROTAC 11β-HSD1 Degrader 1

    		PROTACs 11β-HSD Metabolic Disease
    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) .
    PROTAC 11β-HSD1 Degrader 1
  • HY-120496
    Clofutriben

    ASP3662

    		 11β-HSD Neurological Disease Metabolic Disease
    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 .
    Clofutriben
  • HY-W324243
    11β-HSD1-IN-9

    		11β-HSD Metabolic Disease
    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 .
    11β-HSD1-IN-9
  • HY-14156
    11β-HSD1-IN-15

    		11β-HSD Metabolic Disease
    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 .
    11β-HSD1-IN-15
  • HY-123090
    11β-HSD1-IN-12

    		11β-HSD Metabolic Disease
    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 .
    11β-HSD1-IN-12
  • HY-161449
    JTT-654

    		11β-HSD Metabolic Disease
    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 .
    JTT-654
  • HY-122028
    HSD-016

    		11β-HSD Metabolic Disease
    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 .
    HSD-016
  • HY-W324220
    11β-HSD1-IN-10

    		11β-HSD Metabolic Disease
    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 .
    11β-HSD1-IN-10
  • HY-162026
    11β-HSD1-IN-14

    		11β-HSD Metabolic Disease
    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 .
    11β-HSD1-IN-14
  • HY-145381
    11β-HSD1-IN-6

    		11β-HSD Metabolic Disease
    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 .
    11β-HSD1-IN-6
  • HY-101930
    BMS-816336

    		11β-HSD Metabolic Disease
    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 .
    BMS-816336
  • HY-14393S
    Emodin-d4

    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 . 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 .
    Emodin-d4
  • HY-117428
    INU-101

    		11β-HSD Metabolic Disease
    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 .
    INU-101
  • HY-180549
    11β-HSD1-IN-25

    		11β-HSD AMPK Metabolic Disease
    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 .
    11β-HSD1-IN-25
  • HY-W754031
    11-Dehydrodexamethasone

    		11β-HSD Others
    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 .
    11-Dehydrodexamethasone
  • HY-B1588S
    Carbenoxolone-d4

    		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 . 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 .
    Carbenoxolone-d4
  • HY-112290
    MK-0736

    		11β-HSD Cardiovascular Disease Metabolic Disease
    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 .
    MK-0736
  • HY-10555
    AMG-221

    		11β-HSD Metabolic Disease
    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 .
    AMG-221
  • HY-167696
    11β-HSD1-IN-16

    		11β-HSD Neurological Disease
    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.
    11β-HSD1-IN-16
  • HY-120643
    BMS-823778 hydrochloride

    		11β-HSD Metabolic Disease
    BMS-823778 hydrochloride is a potent, selective and orally active 11β-HSD1 inhibitor with an IC50 of 2.3 nM against human 11β-HSD1 .
    BMS-823778 hydrochloride
  • HY-112290A
    MK-0736 hydrochloride

    		11β-HSD Cardiovascular Disease
    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 .
    MK-0736 hydrochloride
  • HY-101930B
    (R)-BMS-816336

    		11β-HSD Metabolic Disease
    (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 .
    (R)-BMS-816336
  • HY-18054A
    BVT-2733 hydrochloride

    		11β-HSD Inflammation/Immunology
    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 .
    BVT-2733 hydrochloride
  • HY-107124
    BMS-770767

    		11β-HSD Metabolic Disease
    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 .
    BMS-770767
  • HY-178691
    11β-HSD1-IN-24

    		11β-HSD Metabolic Disease
    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 .
    11β-HSD1-IN-24
  • HY-169739
    DG 381B

    		11β-HSD Metabolic Disease
    DG 381B (compound 62) is a 11β-HSD1 and 11β-HSD2inhibitor .
    DG 381B
  • HY-18057
    BVT-3498

    AMG-311

    		 11β-HSD Metabolic Disease
    BVT-3498 (AMG-311) is an inhibitor for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) .
    BVT-3498
  • HY-125421
    11β-HSD1-IN-26

    		11β-HSD Metabolic Disease
    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 .
    11β-HSD1-IN-26
  • HY-117609
    UE2343

    		11β-HSD Neurological Disease
    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 .
    UE2343
  • HY-18054R
    BVT 2733 (Standard)

    		11β-HSD Inflammation/Immunology
    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 .
    BVT 2733 (Standard)
  • HY-W755367
    Methyl glycyrrhetinate

    		11β-HSD Others
    Methyl glycyrrhetinate, a 18b-glycyrrhetinic acid analogue, is a dual inhibitor of 11β-HSD1 and 11β-HSD2 .
    Methyl glycyrrhetinate

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