Ezetimibe (SCH-58235)

N° de catalogueS1655 Lot :S165502

Imprimer

Données techniques

Formule

C24H21F2NO3
Poids moléculaire 409.4 Numéro CAS 163222-33-1
Solubilité (25°C)* In vitro DMSO 82 mg/mL (200.29 mM)
Ethanol 82 mg/mL (200.29 mM)
Water Insoluble
In vivo (Ajouter les solvants au produit individuellement et dans l'ordre.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml signifie légèrement soluble ou insoluble.
* Veuillez noter que Selleck teste la solubilité de tous les composés en interne, et la solubilité réelle peut différer légèrement des valeurs publiées. Ceci est normal et est dû à de légères variations d'un lot à l'autre.
* Expédition à température ambiante (les tests de stabilité montrent que ce produit peut être expédié sans aucune mesure de refroidissement.)

Préparation des solutions mères

Activité biologique

Description Ezetimibe (SCH-58235) est un inhibiteur puissant et sélectif de l'absorption du cholestérol, utilisé pour abaisser le cholestérol.
Cibles
NPC1L1
In vitro Ezetimibe (SCH-58235) produces a significant reduction in total cholesterol, LDL cholesterol, and triglycerides as well as a small but significant increase in HDL cholesterol. This compound reduces cholesterol transport by 31% in Caco-2 cells, but not retinol transport. It 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 (SCH-58235) 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. It 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. This compound 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. It 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. It eliminates exocrine pancreatic function from the intestine while maintaining bile flow, as established in the rat. The compound reduces plasma cholesterol and hepatic cholesterol accumulation in cholesterol-fed hamsters with an ED(50) of 0.04 mg /kg.

Protocole (de référence)

Références

  • https://pubmed.ncbi.nlm.nih.gov/14695813/
  • https://pubmed.ncbi.nlm.nih.gov/16177187/
  • https://pubmed.ncbi.nlm.nih.gov/11742881/
  • https://pubmed.ncbi.nlm.nih.gov/16801428/
  • https://pubmed.ncbi.nlm.nih.gov/11564660/
  • https://pubmed.ncbi.nlm.nih.gov/17587760/

Validation du produit par le client

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 [<sup>3</sup>H]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 [<sup>3</sup>H]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.

Données de [ J Biol Chem , 2014 , 289(19), 12989-99 ]

<p>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.</p>

Données de [ PLoS One , 2012 , 7(12), e51011 ]

Selleck's Ezetimibe (SCH-58235) A été cité par 25 Publications

Modulation of Mitochondria-Endoplasmic Reticulum Contacts (MERCs) by Small Molecules as a New Strategy for Restoring Lipid Metabolism in an Amyotrophic Lateral Sclerosis Model [ J Med Chem, 2025, 68(2):1179-1194] PubMed: 39778888
Discovery of non-steroidal aldo-keto reductase 1D1 inhibitors through automated screening and in vitro evaluation [ Toxicol Lett, 2025, 406:31-37] PubMed: 39988211
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
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

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