Ezetimibe (SCH-58235)

製品コードS1655 バッチS165501

化学情報

	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	82 mg/mL (200.29 mM)
		Ethanol	82 mg/mL (200.29 mM)
		Water	Insoluble
* <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.

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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 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]

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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：

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

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。