Catalog No.
Product Name
Application
Product Information
Citations
- Glucocorticoid that inhibits 11β-hydroxysteroid dehydrogenase (11-HSD) and blocks gap junction communication.
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11β-HSD1 inhibitor
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. -
Necroptosis/11β-HSD1 Inhibitor
Necroptosis-IN-3 is a selective inhibitor of necroptosis, primarily targeting TNF-α induced necroptotic pathways. Additionally, this compound inhibits 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), thereby modulating glucocorticoid metabolism. Its key biological activities make it a valuable tool for researchers studying necroptosis and related cellular mechanisms in various disease models. -
11β-HSD1 Inhibitor
11β-HSD1-IN-25 is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). This compound effectively reduces glucocorticoid levels both in vitro and in serum, while also diminishing lipid accumulation in various models. It modulates lipid metabolism through dual mechanisms involving the inhibition of 11β-HSD1 and activation of the AMP-activated protein kinase (AMPK) signaling pathway. 11β-HSD1-IN-25 is suitable for research applications focused on obesity and related metabolic disorders. -
11β-HSD1 Inhibitor
INCB13739 is a selective and potent inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1), exhibiting an IC50 of 3.2 nM in enzymatic assays and 1.1 nM in peripheral blood mononuclear cells (PBMC). This compound demonstrates significant potential for research in type 2 diabetes mellitus (T2DM) and obesity, targeting the regulation of glucocorticoid metabolism, which plays a critical role in metabolic conditions. Its tissue-specific action makes it a valuable tool for understanding 11β-HSD1-related pathways in metabolic disorders. -
11βHSD Isozymes Inhibitor
11-Beta-hydroxyandrostenedione is an inhibitor of the 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes. This steroid is primarily produced in the adrenal glands and serves as a critical biomarker in differentiating the adrenal from the ovarian sources of hyperandrogenism by measuring plasma levels. Its specificity in inhibiting 11βHSD makes it valuable in endocrine research and the study of steroid biosynthesis pathways. -
11β-HSD1 Inhibitor
11β-HSD1-IN-24 is a potent and selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with an IC50 of 0.5 nM. This compound effectively inhibits the conversion of inactive cortisone to active cortisol, making it a valuable tool for research in metabolic diseases, particularly type 2 diabetes. Its high selectivity and potency position it as an important reagent for studying the physiological roles of glucocorticoids in metabolic pathways. -
11βHSD1 Inhibitor
UE2316 is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1). It has been shown to significantly enhance glucose tolerance and insulin sensitivity in uremic rat models. Additionally, UE2316 has been associated with the exacerbation of hepatic fibrosis in mice. This compound is utilized in research pertaining to metabolic disorders, including hepatic fibrosis, uremia, and diabetes mellitus. -
11β-HSD1 Inhibitor
SKI2852 is a selective, orally active inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), exhibiting IC50 values of 1.6 nM for mouse HSD1 and 2.9 nM for human HSD1. This compound plays a critical role in the modulation of local glucocorticoid metabolism, making it valuable for research focused on metabolic diseases, obesity, and related disorders. Its potent inhibitory activity positions SKI2852 as a significant tool for investigating the physiological and therapeutic implications of 11β-HSD1 modulation. -
11β-HSD Inhibitor
Tetrahydro-11-dehydrocorticosterone is an inhibitor of the 11β-hydroxysteroid dehydrogenase (11β-HSD) enzyme, which plays a critical role in the metabolism of corticosteroids. This compound is utilized in research to study the regulation of glucocorticoid action and its implications in metabolic disorders, stress response, and inflammation. By modulating 11β-HSD activity, it serves as a valuable tool for investigating the therapeutic potential of targeted interventions in hormone-related diseases. -
11β-HSD1 Inhibitor
BMS-770767 is an inhibitor of the enzyme 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1), which is implicated in the pathophysiology of type 2 diabetes. By selectively targeting 11β-HSD1, this compound modulates cortisol availability, influencing metabolic processes in liver and adipose tissue. BMS-770767 is utilized in research focused on obesity, metabolic syndrome, and diabetes-related conditions. -
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. -
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. -
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. -
11β HSD1 Inhibitor
11β-HSD1-IN-8 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β HSD1) with an IC50 value of 2.3 μM against human 11β HSD1. This compound is of significant interest for research into metabolic disorders, particularly diabetes, and its potential impact on cognitive decline. By modulating the enzymatic activity of 11β HSD1, this reagent can facilitate studies aimed at understanding its role in glucocorticoid metabolism and related pathophysiological conditions. -
11β HSD1 Inhibitor
11β-HSD1-IN-7 is a potent inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), demonstrating an IC50 value of 1.9 μM in human enzymatic assays. This compound is valuable for investigating the role of 11β-HSD1 in metabolic disorders such as diabetes and age-related cognitive decline. Its selective inhibition of 11β-HSD1 makes it a useful tool for research into therapeutic strategies targeting these conditions. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
HSD1 Inhibitor
MK-0916 is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (HSD1). This compound induces mechanism-based activation of the hypothalamic-pituitary-adrenal axis, contributing to altered cortisol metabolism. MK-0916 is primarily utilized in research focused on type 2 diabetes and metabolic syndromes, providing insights into glucocorticoid regulation and potential therapeutic interventions. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
11β-HSD2 Inhibitor
18β-Glycyrrhetyl-3-O-sulfate is a potent inhibitor of the enzyme 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), exhibiting an IC50 value of 0.10 µM in rat kidney microsomes. As the principal metabolite of Glycyrrhetinic acid, this compound serves as a substrate for organic anion transporters OAT1 and OAT3. Its anti-inflammatory properties make it a valuable tool for studying pseudohyperaldosteronism and related conditions in biochemical and pharmacological research.
