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    Ezetimibe (SCH 58235)
    Ezetimibe (SCH 58235)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1878
    CAS #: 163222-33-1Purity ≥98%

    Description: Ezetimibe (also known as SCH-58235) is a potent and selective inhibitor of cholesterol absorption in the gut used to lower cholesterol levels. It acts by directly affecting 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 is used clinically to lower plasma cholesterol levels.

    References: J Med Chem. 2004 Jan 1;47(1):1-9; J Nutr. 2005 Oct;135(10):2305-12; Arterioscler Thromb Vasc Biol. 2001 Dec;21(12):2032-8.

    Related CAS#: 1093659-90-5 [Ezetimibe D4 (SCH 58235 D4)]; 191330-56-0 (Ezetimibe ketone; EZM-K); 190448-57-8 (Ezetimibe phenoxy glucuronide); 1376614-99-1 (ent-Ezetimibe; ent-SCH 58235)

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    Molecular Weight (MW)409.4 
    CAS No.163222-33-1 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 82 mg/mL (200.3 mM) 
    Water: <1 mg/mL
    Ethanol: 82 mg/mL (200.3 mM) 
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 10mg/mL 
    SynonymsSCH-58235; SCH 58235; SCH-58235; SCH58235; trade names: Zetia, Ezetrol

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    In Vitro

    In vitro activity: Ezetimibe produces a significant reduction in total cholesterol, LDL cholesterol, and triglycerides as well as a small but significant increase in HDL cholesterol. Ezetimibe reduces cholesterol transport by 31% in Caco-2 cells, but not retinol transport. Ezetimibe results in a significant decrease in mRNA expression for the surface receptors SR-BI, Niemann-Pick type C1 Like 1 protein (NPC1L1), and ATP-binding cassette transporter, subfamily A (ABCA1) and for the nuclear receptors retinoid acid receptor (RAR)gamma, sterol-regulatory element binding proteins (SREBP)-1 and -2, and liver X receptor (LXR)beta as assessed by real-time PCR analysis in Caco-2 cells.

    Kinase Assay: GST-p62 is prepared from Escherichia coli and 0.5 μg of the purified GST-p62 protein is used for in vitro AMPK phosphorylation assay. Phosphorylation of p62 protein by AMPK is determined by non-radioisotope method using γS-ATP. AMPK complex is immuno-purified from the HEK293 cells, to which either myc-AMPKα1 wild-type (WT) or myc-AMPKα1 kinase-dead mutant (KD, D157A) is transfected with Flag-AMPKβ1 and HA-AMPKγ1. AMPK complex is added into the reaction mixture containing 20 mM HEPES, pH7.4, 1 mM EGTA, 0.4 mM EDTA, 5 mM MgCl2, 0.05 mM DTT, 0.5 μg GST-p62, 0.2 mM AMP, and 1 mM ATPγS. Reaction is carried out at 37°C for 30 min, and then terminated by adding 20 mM EDTA. To detect γS-labeled p62 protein, the reaction product is alkylated with 2.5 mM PNBM for 2 h at room temperature and analyzed the products by western blotting using anti-thiophosphate antibody. 

    Cell Assay: In differentiated Caco-2 cells incubated with a carotenoid (1 μM), ezetimibe (10 mg/L) inhibited carotenoid transport with 50% inhibition for ɑ-carotene and β-carotene. Also, it inhibited the transport of β-cryptoxanthin, lycopene and lutein:zeaxanthin(1:1). At the same time, ezetimibe inhibited cholesterol transport by 31%. Ezetimibe decreased the expression of the surface receptors SR-BI, ATP binding cassette transporter, subfamily A (ABCA1), Niemann-Pick type C1 Like 1 protein (NPC1L1) and retinoid acid receptor (RAR)γ, sterol-regulatory element binding proteins SREBP-1 and SREBP-2, and liver X receptor (LXR)β.

    In VivoEzetimibe reduces plasma cholesterol levels from 964 to 374 mg/dL, from 726 to 231 mg/dL, and from 516 to 178 mg/dL in the western, low-fat, and cholesterol-free diet mice, respectively. Ezetimibe reduces aortic atherosclerotic lesion surface area from 20.2% to 4.1% in the western diet group and from 24.1% to 7.0% in the low-fat cholesterol diet mice. Ezetimibe reduces carotid artery atherosclerotic lesion cross-sectional area by 97% in the western and low-fat cholesterol groups and by 91% in the cholesterol-free mice. Ezetimibe inhibits cholesterol absorption, reduces plasma cholesterol, increases high density lipoprotein levels, and inhibits the progression of atherosclerosis under western, low-fat, and cholesterol-free dietary conditions in apoE-/- mice. Ezetimibe potently inhibits the transport of cholesterol across the intestinal wall, thereby reducing plasma cholesterol in preclinical animal models of hypercholesterolemia. Ezetimibe eliminates exocrine pancreatic function from the intestine while maintaining bile flow, is established in the rat. Ezetimibe reduces plasma cholesterol and hepatic cholesterol accumulation in cholesterol-fed hamsters with an ED(50) of 0.04 mg /kg. 
    Animal modelIn apolipoprotein E knockout (apoE-/-) mice, ezetimibe (3 mg/kg) inhibited cholesterol absorption by 90%. Ezetimibe reduced plasma cholesterol, increased HDL levels, and inhibits the progression of atherosclerosis. In phase III human trials, Ezetimibe (10 mg) significantly reduced the levels of LDL cholesterol, total cholesterol and triglycerides and increased the level of HDL cholesterol. 
    Formulation & DosageMice: Ten-week-old C57BL/6J male mice are used. These animals are randomly assigned to one of three groups (7-10 mice in each group): normal chow diet; MCD diet, vehicle-treated; or MCD diet, Ezetimibe -treated. The mice had free access to diet and water, with temperature maintained at 23±2°C, humidity of 60%±10%, and 12-h light/dark cycles. In the MCD diet with Ezetimibe group, Ezetimibe 10 mg/kg is given once daily by oral gavage for 4 weeks. The chow and MCD diet with vehicle groups received the same volume of phosphate buffered saline orally for 4 weeks. Body weight is measured once a week over the course of the treatment period. After 4 weeks, the mice are anesthetized and killed; blood is collected via heart puncture. Tissues are harvested and either snap-frozen in liquid nitrogen and stored at −70°C or fixed in formalin and embedded in paraffin.
    Rats: Male OLETF (n=11) and age-matched LETO rats (n=3) are used, and experiments are conducted in a specific pathogen-free facility with a 12 h light/dark cycle. The OLETF rat is a model that represents late-onset hyperglycemia and exhibits a chronic disease course, mild obesity and clinical onset of diabetes mellitus. Animals have unrestricted access to water and food. At 12 wk of age, rats are randomized and treated with either PBS or Ezetimibe (10 mg/kg per day) via a stomach gavage for 20 wk. At the end of the study, the rats are fasted overnight and anesthetized with intraperitoneal Zoletil/Rompun. Blood is collected from the abdominal aorta, and liver tissues are dissected, immediately frozen in liquid nitrogen, and stored at -80°C until further analysis.
    ReferencesJ Med Chem. 2004 Jan 1;47(1):1-9; J Nutr. 2005 Oct;135(10):2305-12; Arterioscler Thromb Vasc Biol. 2001 Dec;21(12):2032-8. 

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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