Ezetimibe (SCH-58235)

製品コードS1655 バッチS165505

印刷

化学情報

Chemical Structure Synonyms SCH-58235 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H21F2NO3
分子量 409.4 CAS No. 163222-33-1
Solubility (25°C)* 体外 DMSO 81 mg/mL (197.85 mM)
Ethanol 81 mg/mL (197.85 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
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 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Ezetimibe (SCH-58235) is a potent, selective, cholesterol absorption inhibitor, used to lower cholesterol.
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. [1] 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. [2]
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. [3] 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. [4] The compound reduces plasma cholesterol and hepatic cholesterol accumulation in cholesterol-fed hamsters with an ED(50) of 0.04 mg /kg. [5]

プロトコル(参考用のみ)

参考

  • 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/

カスタマーフィードバック

Data from [Data independently produced by J Biol Chem, 2014, 289(19), 12989-99]

Data from [PLoS One, 2012, 7(12), e51011]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。