Ezetimibe依泽替米贝,163222-33-1

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Ezetimibe

CAS No. : 163222-33-1

MCE 国际站：Ezetimibe

产品活性：Ezetimibe (SCH 58235) 是有效的胆固醇吸收 (cholesterol-absorption) 抑制剂。Ezetimibe 是一种 NPC1L1 抑制剂，是有效的 Nrf2 激活剂。

研究领域：NF-κB  |  Autophagy

作用靶点：Keap1-Nrf2  |  Autophagy

In Vitro: Ezetimibe (Eze) acts as a potent Nrf2 activator without causing cytotoxicity. Ezetimibe enhances transactivation of Nrf2, as revealed by a luciferase reporter assay. Ezetimibe also upregulates Nrf2 target genes, including GSTA1, heme oxygenase-1 (HO-1) and Nqo-1 in Hepa1c1c7 and MEF cells. Ezetimibe upregulates Nrf2 target genes in Nrf2+/+ MEF cells, whereas this induction is totally blocked in Nrf2-/- MEF cells. Taken together, Ezetimibe acts as a novel Nrf2 inducer in a ROS-independent manner. Human huh7 hepatocytes are pretreated with Ezetimibe (10 μM, 1 h) and incubated with palmitic acid (PA, 0.5 mM, 24 h) to induce hepatic steatosis. Ezetimibe treatment significantly attenuates PA-increased triglycerides (TG) levels, which is consistent with our animal study. PA treatment resulted in an approximately 20% decrease in mRNA expression of ATG5, ATG6, and ATG7, which had been increased by Ezetimibe treatment. In addition, Ezetimibe treatment significantly increased the PA-induced reduction in LC3 protein abundance.

In Vivo: Administration of Ezetimibe (Eze) reduces the liver weights of mice fed the methionine- and choline-deficient (MCD) diet. This is consistent with the beneficial effects of Ezetimibe on hepatic steatosis. Liver histology shows pronounced multiple macrovesicular fat droplets in mice on the MCD diet, but Ezetimibe treatment markedly decreases the number and size of those droplets. Furthermore, hepatic fibrosis in mice fed the MCD diet is significantly attenuated by Ezetimibe. Blood and liver lipid levels including TG, free fatty acids (FFA), and total cholesterol (TC) are significantly decreased in Ezetimibe-treated OLETF rats. Moreover, OLETF rats show higher serum levels of glucose, insulin, HOMA-IR, TG, FFA, and TC than LETF animals, which are significantly reduced by Ezetimibe. In addition, histological analysis indicated that OLETF control rats showed larger lipid droplets in hepatocytes than age-matched LETO controls, which are attenuated by administration of Ezetimibe.

相关产品：Covalent Screening Library Plus  |  Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  NF-κB Signaling Compound Library  |  Stem Cell Signaling Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Antiviral Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Covalent Screening Library  |  Antioxidant Compound Library  |  Anti-diabetic Compound Library  |  Oxygen Sensing Compound Library  |  Anti-Cardiovascular Disease Compound Library  |  Ferroptosis Compound Library  |  Anti-COVID-19 Compound Library  |  NMPA-Approved Drug Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Anti-Obesity Compound Library  |  Transcription Factor-Targeted Library  |  Lipid Metabolism Compound Library   |  Rare Diseases Drug Library  |  Children’s Drug Library  |  FDA-Approved Anticancer Drug Library  |  Human Metabolite Library  |  Anti-Prostate Cancer Compound Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Non-steroidal Anti-Inflammatory Compound Library  |  Heterocyclic Compound Library  |  Off-patent Drug Library  |  Mitochondrial Toxicity Compound Library  |  Cell Death Library  |  ML385  |  Resveratrol  |  Curcumin  |  4-Octyl itaconate  |  Sulforaphane  |  TBHQ  |  Luteolin  |  Dimethyl fumarate  |  Bardoxolone methyl  |  Omaveloxolone  |  KI696  |  Brusatol  |  Oltipraz  |  Carnosol  |  Hinokitiol  |  Benzbromarone  |  ML334  |  CBR-470-1  |  Mangiferin  |  Astilbin  |  CDDO-Im  |  Pyridoxine hydrochloride  |  Danshensu  |  NK-252  |  Sappanone A  |  Nrf2-IN-1  |  Safranal  |  Eriodictyol

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds