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Technical Data
| Formula | C24H21F2NO3 |
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| Molecular Weight | 409.4 | CAS No. | 163222-33-1 | |
| Solubility (25°C)* | In vitro | DMSO | 81 mg/mL (197.85 mM) | |
| Ethanol | 81 mg/mL (197.85 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Ezetimibe (SCH-58235) is a potent, selective, cholesterol absorption inhibitor, used to lower cholesterol. | |
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| In vitro | Ezetimibe produces a significant reduction in total cholesterol, LDL cholesterol, and triglycerides as well as a small but significant increase in HDL cholesterol. [1] 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. [2] | |
| In vivo | Ezetimibe 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. [3] 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. [4] Ezetimibe reduces plasma cholesterol and hepatic cholesterol accumulation in cholesterol-fed hamsters with an ED(50) of 0.04 mg /kg. [5] |
Protocol (from reference)
References
Customer Product Validation
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Data from [Data independently produced by J Biol Chem, 2014, 289(19), 12989-99]
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Data from [PLoS One, 2012, 7(12), e51011]
Selleck's Ezetimibe (SCH-58235) has been cited by 19 publications
| Inhibition of NPC1L1 disrupts adaptive responses of drug-tolerant persister cells to chemotherapy [ EMBO Mol Med, 2022, 14(2):e14903] | PubMed: 35023619 |
| CircRIC8B regulates the lipid metabolism of chronic lymphocytic leukemia through miR199b-5p/LPL axis [ Exp Hematol Oncol, 2022, 11(1):51] | PubMed: 36064433 |
| The polysaccharide-peptide complex from mushroom Cordyceps militaris ameliorates atherosclerosis by modulating the lncRNA-miRNA-mRNA axis [ Food Funct, 2022, 13(6):3185-3197] | PubMed: 35225320 |
| Development of non-bias phenotypic drug screening for cardiomyocyte hypertrophy by image segmentation using deep learning [ Biochem Biophys Res Commun, 2022, 632:181-188] | PubMed: 36215905 |
| A systems-level study reveals host-targeted repurposable drugs against SARS-CoV-2 infection [ Mol Syst Biol, 2021, 17(8):e10239] | PubMed: 34339582 |
| Polysaccharide CM1 from Cordyceps militaris hinders adipocyte differentiation and alleviates hyperlipidemia in LDLR(+/-) hamsters [ Lipids Health Dis, 2021, 20(1):178] | PubMed: 34895241 |
| Association Between Iron and Cholesterol in Neuroblastomas [ Anticancer Res, 2021, 41(6):2795-2804] | PubMed: 34083269 |
| Ezetimibe promotes CYP7A1 and modulates PPARs as a compensatory mechanism in LDL receptor-deficient hamsters. [ Lipids Health Dis, 2020, 19(1):24] | PubMed: 32035489 |
| Caffeine-free hawk tea lowers cholesterol by reducing free cholesterol uptake and the production of very-low-density lipoprotein. [ Commun Biol, 2019, 2:173] | PubMed: 31098406 |
| Transcriptional control of intestinal cholesterol absorption, adipose energy expenditure and lipid handling by Sortilin. [ Sci Rep, 2018, 8(1):9006] | PubMed: 29899496 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.