11β-HSD Inhibitor

UE2316 is an orally active and specific 11βHSD1 inhibitor. UE2316 significantly improves glucose tolerance and insulin sensitivity in uremic rats. UE2316 also exacerbates hepatic fibrosis in mice. UE2316 can be used in the research of diseases such as hepatic fibrosis, uremia and diabetes mellitus.

BMS-823778 was developed as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 to inhibit type 2 diabetes.

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.

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-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.

BMS-823778 hydrochloride is a potent, selective and orally active 11β-HSD1 inhibitor with an IC₅₀ of 2.3 nM against human 11β-HSD1.

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.

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.

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.

DG 381B (compound 62) is a 11β-HSD1 and 11β-HSD2inhibitor.

3-epi-18β-Glycyrrhetinic acid is an inhibitor of 11β-HSD1 and 11β-HSD2, with an IC₅₀ of 0.17 μM against 11β-HSD2. 3-epi-18β-Glycyrrhetinic acid acts as a weak substrate for sulfotransferase 2A1. It serves as a biomarker for the toxicity of licorice-related pseudoaldosteronism. 3-epi-18β-Glycyrrhetinic acid is applicable to studies related to pseudoaldosteronism.

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.

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.

(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 .

AKR1C3-IN-17 is a cathepsin B (CTSB)-activated small molecule-drug conjugate targeting AKR1C3 with an IC₅₀ of 9 nM. AKR1C3-IN-17 is cleaved by CTSB to release the payload Gemcitabine (HY-17026). AKR1C3-IN-17 induces apoptosis and shows antitumor activity in mice. AKR1C3-IN-17 can be used for the study of hepatocellular carcinoma.

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.

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.

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.

ABT-384 (Standard) is the analytical standard of ABT-384 (HY-111262). This product is intended for research and analytical applications. ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (K_i 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).

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.