For research use only.
CAS No. 163222-33-1
Ezetimibe (SCH-58235) is a potent, selective, cholesterol absorption inhibitor, used to lower cholesterol.
Selleck's Ezetimibe (SCH-58235) has been cited by 13 publications
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Caco-2 cells grown in transwell inserts were transfected with scrambled siRNA, or siRNA specific for CCK1R, CCK2R, or both CCK1 and CCK2R and then incubated with 0.002 uCi of [3H]cholesterol micelles in the apical compartment and with culture medium alone (Control) or 10 nm [Thr28,Nle31]CCK with or without 50 uM ezetimibe (EZ) in the basolateral compartment. Absorbed [3H]cholesterol was determined by radioactivity counting of the basolateral medium. Values represent the mean ± S.E. (error bars) of 4-5 independent experiments. *, p < 0.05 versus control; †, p < 0.05 versus cells treated with CCK alone; ‡, p < 0.05 versus cells transfected with scrambled siRNA alone; $, p < 0.05 versus cells treated with scrambled siRNA and CCK.
J Biol Chem 2014 289(19), 12989-99. Ezetimibe (SCH-58235) purchased from Selleck.
Effect of bile duct ligation, proglumide or ezetimibe on cholecystokinin-elevated plasma cholesterol. LDLR-/- mice were subjected to bile duct ligation (BDL), or intravenous injection of 150 mg/kg proglumide, or were gavage-fed with 5 mg/kg ezetimibe. At 30 min after bile duct ligation, or the administration of proglumide or ezetimibe, mice were intravenously injected with 50 ng/kg of cholecystokinin (CCK) or an equal volume of PBS (control) Blood samples were collected at 2 h after CCK or vehicle injection. Plasma cholesterol was measured with a colorimetric assay. Differences among samples obtained from mice before (control) and after treatment with CCK alone, CCK+BDL, CCK+proglumide or CCK+ezetimibe were analyzed by two-way ANOVA followed by Tukey post-hoc tests. Values represent the mean ± SEM of six independent experiments. *P＜0.05 compared to control, and †P＜0.05 compared to CCK treatment alone.
PLoS One 2012 7(12), e51011. Ezetimibe (SCH-58235) purchased from Selleck.
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|Description||Ezetimibe (SCH-58235) is a potent, selective, cholesterol absorption inhibitor, used to lower cholesterol.|
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. 
|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.  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. |
-  Clader JW, et al. J Med Chem, 2004, 47(1), 1-9.
-  During A, et al. J Nutr, 2005, 135(10), 2305-2312.
-  Davis HR Jr, et al. Arterioscler Thromb Vasc Biol, 2001, 21(12), 2032-2038.
|In vitro||DMSO||81 mg/mL (197.85 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04929249||Recruiting||Drug: Inclisiran||Atherosclerotic Cardiovascular Disease||Novartis Pharmaceuticals|Novartis||June 25 2021||Phase 3|
|NCT04770389||Completed||Drug: Obicetrapib 5mg|Drug: Ezetimibe 10mg|Other: Placebo||Dyslipidemias|High Cholesterol|Hypercholesterolemia||NewAmsterdam Pharma||February 23 2021||Phase 2|
|NCT04762407||Active not recruiting||Drug: HGP1910|Drug: HGP1909|Drug: HCP1903||Healthy||Hanmi Pharmaceutical Company Limited||November 20 2020||Phase 1|
|NCT04643093||Active not recruiting||Drug: Pitavastatin|Drug: Ezetimibe|Drug: 1PC111||Primary Hypercholesterolemia|Mixed Dyslipidemias||Orient Pharma Co. Ltd.||August 1 2020||Phase 3|
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Frequently Asked Questions
I am planning to deliver Ezetimibe per orally and wonder proper vehicle for Ezetimbie and effective dose level for lowering intestinal cholesterol absorption.
S1655 Ezetimibe can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml clearly. If you are going to use this vehicle, please dissolve the drug in DMSO clearly first. Then add PEG 300 and Tween 80, after mixed homogeneously, then dilute with water.