Metabolism

Items 3501-3550 of 6168

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  1. 11β-HSD1 Inhibitor

    ABT-384 is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with exceptional potency, exhibiting high affinity with Ki values ranging from 0.1 to 2.7 nM across rodent, monkey, and human enzyme targets. By preventing the regeneration of active cortisol, ABT-384 serves as a valuable tool in research investigating the pathophysiology of Alzheimer's disease (AD) and related conditions. Its specific action on cortisol metabolism makes it suitable for studies aimed at understanding the role of glucocorticoids in neurodegenerative disorders.
  2. 11β-HSD1 Inhibitor

    (Rac)-BMS-816336 is a potent inhibitor of the 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme, exhibiting IC50 values of 10 nM in human cells and 68 nM in murine cells. Its mechanism of action involves the selective inhibition of 11β-HSD1, leading to modulation of glucocorticoid metabolism. This compound is useful in research applications focused on metabolic disorders, obesity, and conditions associated with dysregulated glucocorticoid action, due to its favorable metabolic stability.
  3. 11β-HSD1 Inhibitor

    HSD-016 is a selective and orally bioavailable inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with IC50 values of 11 nM, 1 nM, and 8 nM against human, mouse, and rat enzymes, respectively. This reagent plays a significant role in studies related to type 2 diabetes by modulating the conversion of inactive cortisone to active cortisol, thereby influencing glucose metabolism and insulin sensitivity. HSD-016 is valuable for investigating the therapeutic potential of 11β-HSD1 inhibition in metabolic disorders.
  4. 11β-HSD Inhibitor

    11β-HSD1-IN-1 is a selective inhibitor of 11β-hydroxydehydrogenase 1 (11β-HSD1) with an IC50 value of 52 nM. It has demonstrated biological activity relevant to modulating corticosteroid metabolism, making it a valuable tool in studies related to various metabolic and inflammatory disorders. This compound is primarily utilized in research applications focused on pain management and related therapeutic areas.
  5. 11β-HSD Inhibitor

    BVT-116429 is a selective inhibitor of 11β-HSD1, a key enzyme involved in cortisol metabolism. This compound has been shown to enhance adiponectin levels and improve glucose homeostasis in diabetic mouse models. In studies involving diabetic KKAy mice, BVT-116429 effectively reduced basal insulin levels and fasting blood glucose levels after 10 days of treatment, demonstrating a potential therapeutic role in the management of metabolic disorders.
  6. 11β-HSD1 Inhibitor

    AMG-221 is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with a Ki value of 12.8 nM as determined by biochemical scintillation proximity assays and an IC50 of 10.1 nM in cell-based assays. This compound demonstrates potential for modulating cortisol metabolism, making it a valuable tool for research into type 2 diabetes and related metabolic disorders.
  7. 11β-HSD1 Inhibitor

    11β-HSD1-IN-9 is a potent inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with IC50 values of 0.48 µM for human and 1.3 µM for murine isoforms. This compound competes with rat 11β-HSD1, making it a valuable tool for investigating the enzyme's role in metabolic disorders. Applications include studies focused on obesity, hyperglycemia, and cognitive impairments, offering insights into the therapeutic potential of targeting 11β-HSD1 in related diseases.
  8. 11β-HSD1 Inhibitor

    11β-HSD1-IN-12 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), a crucial enzyme that converts inactive glucocorticoids to their active forms, thereby influencing intracellular glucocorticoid levels. This compound is significant in research related to obesity and metabolic syndrome, providing a valuable tool for studying the therapeutic potential of modulating glucocorticoid metabolism.
  9. 11β-HSD1 Inhibitor

    11β-HSD1-IN-11 is a competitive inhibitor of 11β-HSD1, exhibiting IC50 values of 0.34 μM for rat and 0.13 μM for human enzymes. This compound effectively modulates cortisol metabolism, thereby influencing glucocorticoid signaling pathways. It is useful for studying the role of 11β-HSD1 in metabolic disorders and other physiological processes.
  10. 11β-HSD1 Inhibitor

    11β-HSD1-IN-10 is a potent inhibitor of the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), with an IC50 of 1.8 µM in human models. This compound is valuable for research on obesity, hyperglycemia, and cognitive impairment, providing insights into metabolic regulation and endocrine function. Its effectiveness makes it a useful tool for studying the role of glucocorticoid metabolism in various physiological and pathological conditions.
  11. 11β-HSD Inhibitor

    BMS-823778 is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1, which plays a crucial role in the regulation of cortisol metabolism. This compound has demonstrated potential in modulating glucose homeostasis and is primarily investigated for its applications in type 2 diabetes research. The inhibition of 11β-HSD1 by BMS-823778 may aid in exploring therapeutic strategies for metabolic disorders and related conditions.
  12. CYP17A1 Substrate

    11-Ketoprogesterone (11KP4) serves as a substrate for the enzymes CYP17A1 and 11β-HSD2, facilitating the conversion to 21-deoxycortisone (21dE) and 21-deoxycortisol (21dF), both of which exhibit glucocorticoid activity. This compound is pivotal for studies examining steroidogenesis and adrenal hormone metabolism. It is utilized in research applications focusing on hormonal regulation and related disorders, providing insights into steroid hormone biosynthesis pathways.
  13. 11β-HSD1 Inhibitor

    MK-0736 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), which plays a critical role in cortisol metabolism. This compound has been shown to lower blood pressure and is instrumental in research on type 2 diabetes and metabolic syndrome. Its application may support investigations into the therapeutic potential for managing metabolic disorders and related cardiovascular conditions.
  14. 11β-HSD-1 Inhibitor

    11β-HSD1-IN-6 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1), which catalyzes the conversion of active glucocorticoids such as cortisol to their inactive forms, 11-dehydrocorticosterone or cortisone. By inhibiting this enzyme, 11β-HSD1-IN-6 can modulate glucocorticoid availability and has potential applications in studies related to metabolic disorders, stress response, and associated therapeutic strategies. This compound serves as a valuable tool for investigating the biological roles of glucocorticoids and their implications in various diseases.
  15. 11β-HSD1 Inhibitor

    BMS-823778 hydrochloride is a selective and potent 11β-HSD1 inhibitor, exhibiting an IC50 of 2.3 nM against human 11β-HSD1. This compound plays a crucial role in regulating cortisol metabolism and glucose homeostasis, making it valuable in research related to metabolic disorders, obesity, and diabetes. It is particularly useful for studies investigating the effects of 11β-HSD1 inhibition on insulin sensitivity and related pathways.
  16. 11β-HSD1 Inhibitor

    UE2343 is a potent inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), which plays a critical role in glucocorticoid metabolism. This compound is designed for oral administration and exhibits the ability to penetrate the blood-brain barrier. UE2343 is being researched for its potential therapeutic effects in the treatment of Alzheimer's disease, targeting neuroinflammation and cognitive decline associated with the condition.
  17. 11β-HSD1 Inhibitor

    BI-135585 hydrate is a selective and potent inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) with an IC50 of 13 nM. This compound demonstrates greater than 1000-fold selectivity over other hydroxysteroid dehydrogenases, making it a valuable tool for research. BI-135585 hydrate is primarily employed in studies related to type 2 diabetes, where modulation of glucocorticoid metabolism is of interest.
  18. 11β-HSD1/11β-HSD2 Inhibitor

    DG 381B is a selective inhibitor of 11β-HSD1 and 11β-HSD2, enzymes involved in the regulation of glucocorticoid metabolism. By inhibiting these enzymes, DG 381B plays a significant role in modulating cortisol levels, which can impact metabolic processes and inflammatory responses. This compound is valuable for research applications related to metabolic diseases, hypertension, and other conditions associated with glucocorticoid action.
  19. 11β-HSD1 Inhibitor

    MK-0736 hydrochloride is a potent and selective inhibitor of 11β-HSD1, a key enzyme involved in glucocorticoid metabolism. This compound has shown significant antihypertensive effects and is valuable for research into metabolic syndrome and related disorders. Clinical studies indicate that MK-0736 hydrochloride possesses a favorable safety profile, making it a promising candidate for further exploration in hypertension-related research.
  20. 11β-HSD1 Inhibitor

    INU-101 is a selective, orally active inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). It demonstrates potent inhibitory activity in liver microsomes from mouse, monkey, and human sources, effectively enhancing insulin sensitivity and reducing fasting blood glucose levels. This compound is applicable in research focused on metabolic diseases, particularly diabetes, making it a valuable tool for studying metabolic pathways and potential therapeutic strategies.
  21. 11β-HSD1 Inhibitor

    (R)-BMS-816336 is a selective inhibitor of the 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme. It demonstrates potent inhibitory activity with IC50 values of 14.5 nM for human, 50.3 nM for mouse, and 16 nM for cynomolgus monkey 11β-HSD1. This compound is applicable in research focused on metabolic disorders, obesity, and diabetes due to its role in modulating glucocorticoid metabolism.
  22. 11β-HSD Inhibitor

    Clofutriben (ASP3662) is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). By inhibiting this enzyme, Clofutriben plays a critical role in modulating cortisol metabolism, thereby influencing glucocorticoid signaling pathways. This compound is primarily utilized in research related to metabolic disorders, obesity, and stress response. Its applications include evaluating the therapeutic potential of targeting 11β-HSD1 in various disease models.
  23. 11β-HSD Inhibitor

    11β-HSD1-IN-16 is a selective inhibitor of the 11β-hydroxysteroid dehydrogenase HSD11B1, with an IC50 of 0.34 μM. This compound has key applications in research related to neuropathic pain, inflammatory pain, and occipital neuralgia. Its ability to modulate glucocorticoid metabolism makes it an important tool for understanding the role of 11β-HSD in various pain pathways.
  24. 11β-HSD1 Inhibitor

    11β-HSD1-IN-15 is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type I (11β-HSD1), effectively blocking the conversion of corticosterone to cortisol. By binding to the enzyme's active site, it serves as a valuable tool for investigating the role of 11β-HSD1 in various pathological conditions. This compound is particularly relevant for research on metabolic syndrome, obesity, cognitive decline, and type 2 diabetes, enabling insights into therapeutic strategies targeting these disorders.
  25. 11β-HSD Inhibitor

    11β-HSD1-IN-14 is a selective inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) with an IC50 of 74 nM for human HSD1 and 603 nM for HSD1 expressed in HEK293 cells. This compound demonstrates significant potential for modulating cortisol metabolism, making it relevant for research in metabolic disorders, obesity, and stress-related conditions. Its specificity supports studies aimed at elucidating the role of 11β-HSD1 in various physiological and pathological processes.
  26. 11β-HSD1 Inhibitor

    JTT-654 is a potent and selective inhibitor of 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1), exhibiting an IC50 of 4.65 nM for the human enzyme. This compound acts competitively against human recombinant 11β-HSD1 while demonstrating minimal inhibition of 11β-HSD2 (IC50 > 30 μM). JTT-654 has been shown to improve insulin resistance and alleviate non-obese type 2 diabetes by targeting 11β-HSD1 in adipose tissue and the liver, making it a valuable tool for studying metabolic disorders.
  27. 11β-HSD1 Inhibitor

    BVT-2733 hydrochloride is a selective, nonsteroidal inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). With an IC50 of 96 nM for the mouse enzyme, it exhibits lower potency against the human variant (IC50 of 3341 nM). This compound is valuable for investigating the role of 11β-HSD1 in the pathophysiology of arthritis and obesity-related conditions, providing insights into therapeutic strategies for these diseases.
  28. 11β-HSD Inhibitor

    BVT-3498 is a potent inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), a key enzyme in glucocorticoid metabolism. By selectively blocking 11β-HSD1 activity, BVT-3498 modulates local cortisol levels, which is critical for research into metabolic diseases and stress-related disorders. This compound serves as a valuable tool in elucidating the role of 11β-HSD1 in various physiological and pathological processes.
  29. 15-PGDH Inhibitor

    MF-DH-300 is a selective inhibitor of 15-PGDH, a key enzyme in the degradation of prostaglandins. By inhibiting this enzyme, MF-DH-300 enhances prostaglandin levels, which may have therapeutic implications in muscle disorders, such as spinal muscular atrophy (SMA). This compound is valuable for research focused on understanding the role of prostaglandins in muscle-related pathologies and developing potential interventions.
  30. 15-PGDH Inhibitor

    ML148 is a potent and selective inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH), exhibiting an IC50 of 56 nM. This compound is particularly valuable for the investigation of prostaglandin signaling pathways, which play critical roles in inflammation, pain, and various physiological processes. ML148’s specificity and inhibitory capacity make it a crucial tool for exploring the modulation of prostaglandin metabolism in various biological contexts.
  31. 15-PGDH Inhibitior

    15-PGDH-IN-1 is a potent inhibitor of the enzyme 15-hydroxyprostaglandin dehydrogenase (15-PGDH) with an IC50 value of 3 nM against recombinant human 15-PGDH. This compound is orally active and is valuable for investigating the roles of 15-PGDH in tissue repair and regeneration processes. Its inhibitory action may facilitate research into therapeutic strategies targeting inflammation and cellular regeneration.
  32. 15-PGDH Inhibitor

    HW201877 is an effective and orally active inhibitor of 15-prostaglandin dehydrogenase (15-PGDH) with an IC50 value of 3.6 nM. This compound significantly increases PGE2 levels in A549 cells and has demonstrated notable efficacy in preclinical models of tissue injury and fibrosis. HW201877 is suitable for investigating inflammatory bowel disease (IBD), idiopathic pulmonary fibrosis (IPF), and Crohn’s disease (CD).
  33. 15-PGDH Inhibitor

    15-PGDH-IN-4 is a potent inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH), exhibiting an IC50 value of 1.2 nM against human 15-PGDH. This reagent is valuable for research into immune cell function and tissue regeneration, enabling the exploration of metabolic pathways and inflammatory processes. Its ability to modulate 15-PGDH activity makes it a critical tool for studies aimed at understanding and manipulating prostaglandin signaling.
  34. 15-PGDH Inhibitor

    (R)-SW033291 is a potent and high-affinity inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH). By inhibiting this enzyme, (R)-SW033291 significantly increases levels of prostaglandin E2 (PGE2) in bone marrow and other tissues. This compound has potential applications in research focused on tissue regeneration and the modulation of inflammatory responses associated with prostaglandin signaling.
  35. 15-PGDH Inhibitor

    MF-PGDH-008 is a selective inhibitor of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase (15-PGDH). This compound plays a crucial role in modulating prostaglandin levels, offering significant potential in research focused on inflammation and cancer biology. Its ability to inhibit 15-PGDH makes it valuable for exploring therapeutic strategies aimed at enhancing prostaglandin signaling in various biomedical studies.
  36. 15-PGDH Inhibitor

    15-PGDH-IN-3 is a selective competitive inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH). This compound plays a critical role in regulating prostaglandin levels and can be utilized to study the modulation of inflammatory responses and cancer progression. Its inhibition of 15-PGDH may have implications in various research applications, including pain management and the investigation of therapeutic targets in oncology.
  37. 15-PGDH Inhibitor

    CAY10397 is a selective and orally bioavailable inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH). It effectively inhibits the production of endogenous metabolites dependent on 15-PGDH, and it has been shown to block selenium-dependent protective mechanisms in inflammation. CAY10397 is primarily utilized in research related to colitis and other inflammatory conditions, providing insights into the role of 15-PGDH in disease pathology.
  38. 15-PGDH Inhibitor

    15-epi-PGE1 is a stereoisomer of Prostaglandin E1 that functions as a non-competitive inhibitor of human placental 15-Hydroxyprostaglandin dehydrogenase (15-PGDH). With an IC50 value of 170 μM, this compound exhibits inhibitory activity that can be utilized in studies of prostaglandin metabolism. Research applications may include investigations into the roles of prostaglandins in various physiological and pathological processes.
  39. 15-PGDH Inhibitor

    15-PGDH-IN-2 is a potent inhibitor of 15-PGDH, displaying an IC50 value of 0.274 nM. This compound is valuable for researching biological processes such as hair loss, bone formation, gastric ulcer healing, and dermal wound healing. Its ability to modulate 15-PGDH activity makes it a useful tool in studying pathways associated with these conditions.
  40. 17β-HSD1 Inhibitor

    17β-HSD1-IN-1 is a selective inhibitor of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1), exhibiting IC50 values of 5.6 nM for 17β-HSD1 and 3155 nM for 17β-HSD2. This compound plays a crucial role in modulating estrogen levels and is pertinent for research focused on non-small cell lung cancer (NSCLC). Its specificity enables targeted studies into the enzymatic pathways associated with hormone-driven tumorigenesis.
  41. 17β-HSD10 Inhibitor

    17β-HSD10-IN-1 is a potent inhibitor of 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10), exhibiting oral bioavailability and effective blood-brain barrier penetration. This compound is characterized by a selective mechanism of action that minimizes off-target effects on mitochondria, along with a favorable safety profile devoid of cytotoxic or neurotoxic effects. It is suitable for research applications focused on disorders related to steroid metabolism and neurodegenerative diseases.
  42. 17β-HSD10 Inhibitor

    17β-HSD10-IN-2 is a selective inhibitor of 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10), a multifunctional enzyme located in the mitochondria. This compound demonstrates significant inhibition of 17β-HSD10 without causing off-target effects on mitochondrial function or exhibiting cytotoxic and neurotoxic properties. 17β-HSD10-IN-2 is valuable for research applications focused on Alzheimer's disease and hormone-dependent cancers, facilitating the exploration of therapeutic strategies targeting this enzyme.
  43. 17β-HSD5 Inhibitor

    17β-HSD5 Inhibitor 3 is a selective inhibitor of the enzyme 17β-HSD5, exhibiting an IC50 value of 69 nM. This compound plays a crucial role in modulating steroid metabolism and can be utilized in research related to steroid-related disorders and hormonal regulation. Its oral bioactivity makes it a valuable tool for exploring therapeutic approaches in conditions influenced by 17β-HSD5 activity.
  44. 17β-HSD10 Inhibitor

    17β-HSD10-IN-3 is a selective inhibitor of 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10) with an IC50 value of 5.59 μM. This compound demonstrates a lack of cytotoxicity in the HEK-293 cell line at concentrations up to 20 μM. It is suited for research applications investigating the role of 17β-HSD10 in steroid metabolism and neurodegenerative diseases.
  45. 17β-HSD3 Inhibitor

    BMS-856 is a selective inhibitor of 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3). It demonstrates potent inhibitory activity with IC50 values of 60 nM in enzyme assays and 300 nM in whole cell assays, effectively disrupting the enzyme's activity. BMS-856 is valuable for research focused on steroidogenesis and potential therapeutic applications in hormonal disorders, particularly those related to testosterone metabolism.
  46. 17β-HSD3 Inhibitor

    SCH-451659 is a selective inhibitor of 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) with an IC50 of 2.4 nM. By blocking the conversion of androstenedione to testosterone, SCH-451659 effectively lowers testosterone levels in vivo. This compound exhibits potential anticancer activity, particularly against prostate tumors that depend on androstenedione. Its specific targeting mechanism makes SCH-451659 a valuable reagent for research in hormone-related cancer therapies.
  47. 17β-HSD Inhibitor

    HSD17B13-IN-17 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting IC50 values of less than 0.1 μM for estradiol and under 1 μM for Leukotriene B3. This compound is significant in the study of nonalcoholic fatty liver diseases (NAFLDs), including nonalcoholic steatohepatitis (NASH). HSD17B13-IN-17 is essential for research focused on the modulation of lipid metabolism and the therapeutic potential of HSD17B13 inhibitors in liver-related disorders.
  48. 17β-HSD Inhibitor

    HSD17B13-IN-27 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC50 of less than 0.1 μM for estradiol and less than 1 μM for leukotriene B3. This compound is instrumental in research involving nonalcoholic fatty liver diseases (NAFLD), including nonalcoholic steatohepatitis (NASH). Its ability to modulate steroid hormone metabolism positions it as a valuable tool for studying metabolic disorders and developing therapeutic strategies.
  49. 17β-HSD Inhibitor

    HSD17B13-IN-19 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), demonstrating an IC50 of less than 0.1 μM for estradiol and below 1 μM for leukotriene B3. This compound is significant in the context of nonalcoholic fatty liver diseases (NAFLDs), including nonalcoholic steatohepatitis (NASH). Its inhibition of HSD17B13 may provide insights into therapeutic strategies for managing liver-related metabolic disorders.
  50. 17β-HSD5 Inhibitor

    EM 1404 is a potent inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17β-HSD5) with an IC50 of 3.2 nM. This compound plays a crucial role in modulating androgen metabolism and has significant implications in the study of hormone-related disorders. EM 1404 is valuable for research focused on exploring therapeutic strategies for conditions associated with altered steroid hormone levels.

Items 3501-3550 of 6168

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