2. Vías de señalización
  3. Metabolic Enzyme/Protease
  4. 11β-HSD
  5. 11β-HSD Inhibitor

11β-HSD Inhibitor

11β-HSD Inhibitors (64):

Cat. No. Nombre del producto Efecto Pureza
  • HY-B1588S
    Carbenoxolone-d4
    		Inhibitor 99.28%
    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.
  • HY-112290
    MK-0736
    		Inhibitor
    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.
  • HY-145381
    11β-HSD1-IN-6
    		Inhibitor
    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.
  • HY-180549
    11β-HSD1-IN-25
    		Inhibitor
    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.
  • HY-120643
    BMS-823778 hydrochloride
    		Inhibitor
    BMS-823778 hydrochloride is a potent, selective and orally active 11β-HSD1 inhibitor with an IC50 of 2.3 nM against human 11β-HSD1.
  • HY-123181
    MK-0916
    		Inhibitor
    MK-0916 is a HSD1 inhibitor. MK-0916 produces mechanism-based activation of the hypothalamic-pituitary-adrenal axis. MK-0916 can be used in the research of type 2 diabetes and metabolic syndromes.
  • HY-117609
    UE2343
    		Inhibitor
    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.
  • HY-105286A
    BI-135585 hydrate
    		Inhibitor
    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.
  • HY-169739
    DG 381B
    		Inhibitor
    DG 381B (compound 62) is a 11β-HSD1 and 11β-HSD2inhibitor.
  • HY-112290A
    MK-0736 hydrochloride
    		Inhibitor
    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.
  • HY-117428
    INU-101
    		Inhibitor
    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.
  • HY-101930B
    (R)-BMS-816336
    		Inhibitor
    (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 .
  • HY-105286
    BI-135585
    		Inhibitor
    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.
  • HY-18056R
    PF-915275 (Standard)
    		Inhibitor
    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.
  • HY-14156
    11β-HSD1-IN-15
    		Inhibitor
    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.
  • HY-18054R
    BVT 2733 (Standard)
    		Inhibitor
    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.
  • HY-162026
    11β-HSD1-IN-14
    		Inhibitor
    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.
  • HY-183905
    KR-67607
    		Inhibitor
    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.
  • HY-161449
    JTT-654
    		Inhibitor
    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.
  • HY-W755367
    Methyl glycyrrhetinate
    		Inhibitor
    Methyl glycyrrhetinate, a 18β-glycyrrhetinic acid analogue, is a dual inhibitor of 11β-HSD1 and 11β-HSD2.