Ezetimibe

CAS No. 163222-33-1

Ezetimibe( Ezetrol | SCH 58235 )

Catalog No. M12456 CAS No. 163222-33-1

A potent Niemann-Pick C1-Like 1 (NPC1L1) cholesterol absorption receptor inhibitor that inhibits sterol absorption without affecting the absorption of other molecules.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Ezetimibe
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent Niemann-Pick C1-Like 1 (NPC1L1) cholesterol absorption receptor inhibitor that inhibits sterol absorption without affecting the absorption of other molecules.
  • Description
    A potent Niemann-Pick C1-Like 1 (NPC1L1) cholesterol absorption receptor inhibitor that inhibits sterol absorption without affecting the absorption of other molecules; significantly reduces plasma levels of total and low density lipoprotein cholesterol (LDL-C) both in vitro and in vivo; also is a potent Nrf2 activator that protects mice from diet-induced nonalcoholic steatohepatitis; increases autophagic flux, improves hepatic steatosis in obese and diabetic rats.Hypercholesterolemia Approved(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.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    Ezetrol | SCH 58235
  • Pathway
    Nuclear Receptor/Transcription Factor
  • Target
    Keap1-Nrf2
  • Recptor
    NPC1L1|Nrf2|SterolO-acyltransferase
  • Research Area
    Cardiovascular Disease
  • Indication
    Hypercholesterolemia

Chemical Information

  • CAS Number
    163222-33-1
  • Formula Weight
    409.4252
  • Molecular Formula
    C24H21F2NO3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 29 mg/mL
  • SMILES
    O=C1N(C2=CC=C(F)C=C2)[C@H](C3=CC=C(O)C=C3)[C@H]1CC[C@@H](C4=CC=C(F)C=C4)O
  • Chemical Name
    2-Azetidinone, 1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)-, (3R,4S)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Pirillo A, et al. Curr Med Chem. 2016;23(10):983-99. 2. Chang E, et al. World J Gastroenterol. 2015 Jul 7;21(25):7754-63. 3. Lee DH, et al. Free Radic Biol Med. 2016 Oct;99:520-532.
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