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Results for "

rat 11β-HSD1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (7) Endogenous Metabolite (1)
By Research Areas:	Cancer (1) Inflammation/Immunology (1) Metabolic Disease (6) Neurological Disease (2)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 K_i of 35.8 μM against human *11β-HSD1, and an IC₅₀* of 17.39 μM and a K_i 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 .

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 .

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 K_i 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 .

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 .

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 .

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 .

HY-W755367

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

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-124529

Lunularin	Structural Classification Human Gut Microbiota Metabolites other families Conocephalum conicum (L.) Dumort. Phenols Polyphenols Plants Endogenous metabolite Source Classification	11β-HSD Endogenous Metabolite
Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1, with an IC₅₀ of 45.44 μM and a K_i of 35.8 μM against human *11β-HSD1, and an IC₅₀* of 17.39 μM and a K_i 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 .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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rat 11β-HSD1

Inhibitors & Agonists

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