Date published: 2026-4-24

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Ezetimibe (CAS 163222-33-1)

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Alternate Names:
Zetia
Application:
Ezetimibe is a cholesterol transport inhibitor that binds to NPC1L1
CAS Number:
163222-33-1
Purity:
≥99%
Molecular Weight:
409.43
Molecular Formula:
C24H21F2NO3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Ezetimibe has been reported to be a cholesterol transport inhibitor. Mechanistic studies show that this compound directly affects Niemann-Pick C1-like 1 (NPC1L1) and prevents it from incorporating into clathrin-coated vesicles. NPC1L1 is a polytopic transmembrane protein that facilitates absorption of cholesterol via clathrin/AP2-mediated endocytosis. By binding to NPC1L1, ezetimibe prevents endocytosis of this protein therefore blocking cholesterol transfer across membranes.


Ezetimibe (CAS 163222-33-1) References

  1. Ezetimibe-induced hyperlipidaemia.  |  Doherty, E., et al. 2005. Int J Clin Pract Suppl. 3-5. PMID: 15875607
  2. Ezetimibe ameliorates cholecystosteatosis.  |  Mathur, A., et al. 2007. Surgery. 142: 228-33. PMID: 17689690
  3. Ezetimibe and simvastatin reduce inflammation, disease activity, and aortic stiffness and improve endothelial function in rheumatoid arthritis.  |  Mäki-Petäjä, KM., et al. 2007. J Am Coll Cardiol. 50: 852-8. PMID: 17719471
  4. The cholesterol absorption inhibitor ezetimibe acts by blocking the sterol-induced internalization of NPC1L1.  |  Ge, L., et al. 2008. Cell Metab. 7: 508-19. PMID: 18522832
  5. Ezetimibe in diabetes: more than cholesterol lowering?  |  Sarigianni, M., et al. 2010. Curr Med Res Opin. 26: 2517-20. PMID: 20843163
  6. Ezetimibe and vascular endothelial function.  |  Ikeda, S. and Maemura, K. 2011. Curr Vasc Pharmacol. 9: 87-98. PMID: 21044017
  7. Ezetimibe and low density lipoprotein subfractions: an ongoing debate.  |  Katsiki, N., et al. 2011. Curr Med Res Opin. 27: 693-5. PMID: 21275848
  8. Aminolysis of ezetimibe.  |  Baťová, J., et al. 2015. J Pharm Biomed Anal. 107: 495-500. PMID: 25686539
  9. Liver Injury Associated With Ezetimibe Monotherapy.  |  Kanagalingam, T., et al. 2021. CJC Open. 3: 195-197. PMID: 33644733
  10. Synthesis and Modeling of Ezetimibe Analogues.  |  Salgado, MM., et al. 2021. Molecules. 26: PMID: 34067439
  11. Ezetimibe Prevents IL-1β-induced Inflammatory Reaction in Mouse Chondrocytes via Modulating NF-κB and Nrf2/HO-1 Signaling Crosstalk.  |  Weng, Q., et al. 2022. Curr Pharm Biotechnol. 23: 1772-1780. PMID: 34983342
  12. Preformulation Studies of Ezetimibe-Simvastatin Solid Dispersions in the Development of Fixed-Dose Combinations.  |  Górniak, A., et al. 2022. Pharmaceutics. 14: PMID: 35631498
  13. Ezetimibe ameliorates clinical symptoms in a mouse model of ankylosing spondylitis associated with suppression of Th17 differentiation.  |  Moon, J., et al. 2022. Front Immunol. 13: 922531. PMID: 36059546

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Ezetimibe, 25 mg

sc-205690
25 mg
$96.00

Ezetimibe, 100 mg

sc-205690A
100 mg
$241.00

What is the appearance of the chemical?

Asked by: two2igm05
Thank you for your question. The compound, sc-205690, is provided as a white crystalline powder. If you have any further questions or concerns, please feel free to contact our Technical Service department by calling 800-457-3801 option 2, emailing scbt@scbt.com. or using the Live Chat function on our website.
Answered by: Tech Service 8
Date published: 2023-09-14
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Rated 5 out of 5 by from Works fineHave been trying it out lately...will have to check results shortly
Date published: 2017-10-16
Rated 5 out of 5 by from Dalb geDalb ge, LS. et al. (PubMed 26266945) found that treatment with Ezetimibe, a cholesterol transport inhibitor that affects NPC1L1 and prevents its incorporation into membrane clathrin-coated vesicles, in hyperlipidemic diet-induced obesity hamsters, for 14 days resulted in lower cholestreol in plasma with a marked decline in LDL levels. -SCBT Publication Review
Date published: 2015-02-23
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Ezetimibe is rated 5.0 out of 5 by 2.
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