Ezetimibe

SKU: orb1308079

Description

Ezetimibe (SCH 58235) is a potent and selective inhibitor of dietary cholesterol absorption, acting locally within the intestinal brush border. This small molecule is widely used in research to investigate lipid metabolism, atherosclerosis, and metabolic diseases in both in vitro cellular assays and in vivo animal models.

Research Area

Cell Biology, Neuroscience

Key Properties

• CAS Number: 163222-33-1
• MW: 409.43
• Purity: >98%
• Formula: C₂₄H₂₁F₂NO₃
• SMILES: C(C[C@H](O)C1=CC=C(F)C=C1)[C@@H]2[C@H](N(C2=O)C3=CC=C(F)C=C3)C4=CC=C(O)C=C4
• Target: Inflammasome
• Solubility: Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 15 mg/ml).

Bioactivity

• In Vivo:
  Ezetimibe significantly reduces the expression of mRNA for scavenger receptor class B type I (SR-BI), Niemann-Pick C1-like 1 protein (NPC1L1), ATP-binding cassette transporters, sub-family A member (ABCA), the β subunit of liver X receptor (LXRβ), retinoid X receptor γ (RXRγ), and steroid regulatory element-binding proteins 1 and 2 (SREBP-1 and -2). Ezetimibe notably decreases total cholesterol, low-density lipoprotein (LDL) cholesterol, and triglycerides, while moderately increasing high-density lipoprotein (HDL) cholesterol levels. In Caco-2 cells, Ezetimibe reduces cholesterol transport by 31% without affecting retinol transport.
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• In Vitro:
  Ezetimibe effectively inhibits the transport of cholesterol across the intestinal wall, thereby reducing plasma cholesterol in preclinical animal models of hypercholesterolemia. It eliminates exocrine pancreatic function in rats while maintaining bile flow. In hamsters fed with cholesterol, ezetimibe reduces plasma cholesterol and hepatic cholesterol accumulation, with an effective dose (ED50) of 0.04 mg/kg. It also decreases the surface area of aortic atherosclerotic lesions, from 20.2% in the control group to 4.1% in the group on a Western diet and 7.0% in mice on a low-fat cholesterol diet. Furthermore, ezetimibe reduces the cross-sectional area of carotid atherosclerotic lesions by 97% in the Western low-fat cholesterol diet group and by 91% in cholesterol-free mice.
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• Cell Research:
  Ezetimibe is dissolved in DMSO and stored, and then diluted with appropriate medium before use. Huh7 human hepatocytes are cultured in high glucose DMEM containing 10% FBS, 100 units/mL penicillin and 100 μg/mL streptomycin at 37°C in a 95% air/5% CO2 atmosphere. Hepatocytes are treated with or without Ezetimibe (10 μM, 1 h) and incubated with palmitic acid (PA, 0.5 mM, 24 h).
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Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SCH 58235; Ezetrol

Compound Identifiers

PubChem CID

150311