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11β-HSD inhibitor

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Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B1367
    Carbenoxolone disodium
    3 Publications Verification

    Gap Junction Protein Orthopoxvirus 11β-HSD Infection Inflammation/Immunology
    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.
    Carbenoxolone disodium
  • HY-W106057

    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-W129359

    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-W588255

    11β-HSD Metabolic Disease
    Tetrahydro-11-dehydrocorticosterone is a 11β-HSD inhibitor .
    Tetrahydro-11-dehydrocorticosterone
  • HY-112290

    11β-HSD 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-151627

    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-W324243

    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-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-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-157161

    11β-HSD Cancer
    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 .
    11β-HSD2-IN-1
  • HY-145381

    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-W324220

    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-U00325

    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-120643

    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-161449

    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-18173

    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-150701

    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-162026

    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-107124

    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-123800

    VTP-34072

    11β-HSD Neurological Disease
    BI 187004 (VTP-34072) is an 11β-hydroxysteroid dehydrogenase 1 inhibitor for use in diabetes research .
    BI 187004
  • HY-122028

    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-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

    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-18057

    AMG-311

    11β-HSD Metabolic Disease
    BVT-3498 (AMG-311) is an inhibitor for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) .
    BVT-3498
  • HY-111262

    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-148454

    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-14393
    Emodin
    Maximum Cited Publications
    21 Publications Verification

    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-101930

    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-160618

    11β-HSD Metabolic Disease
    11β-HSD2-IN-2 (compound 3) is a selective inhibitor for 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) with an IC50 of 300 nM .
    11β-HSD2-IN-2
  • HY-117609

    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-14393S

    Frangula emodin-d4

    Isotope-Labeled Compounds SARS-CoV Casein Kinase Autophagy 11β-HSD Cancer
    Emodin-d4 is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice[3].
    Emodin-d4
  • HY-14393R

    Frangula emodin (Standard)

    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

    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-112290A

    11β-HSD Others 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

    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-10555

    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-105286

    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-18054
    BVT 2733
    3 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-101930A

    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-114464S

    4-Androsten-11β-ol-3,17-dione-d4

    Isotope-Labeled Compounds Endogenous Metabolite 11β-HSD Endocrinology
    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[1][2].
    11-Beta-hydroxyandrostenedione-d4
  • HY-114464

    4-Androsten-11β-ol-3,17-dione

    Endogenous Metabolite 11β-HSD Endocrinology
    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 .
    11-Beta-hydroxyandrostenedione
  • HY-114464S1

    4-Androsten-11β-ol-3,17-dione-d7

    Endogenous Metabolite 11β-HSD Others
    11-Beta-hydroxyandrostenedione-d7 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor [1][2]
    11-Beta-hydroxyandrostenedione-d7
  • HY-148682

    Glycyrrhetic acid 3-O-hydrogen sulfate

    OAT 11β-HSD Drug Metabolite Metabolic Disease Inflammation/Immunology
    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 .
    18β-Glycyrrhetyl-3-O-sulfate
  • HY-B1588S

    Amyloid-β HIV 11β-HSD Infection Neurological Disease Inflammation/Immunology
    Carbenoxolone-d4 is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties[3]. Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease[2]. Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD[1]. Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop[4].Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself[6].
    Carbenoxolone-d4

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