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Postion:Product Catalog >API>Circulatory system drugs>Anti-atherosclerotic Drugs>Ezetimibe
Ezetimibe
  • Ezetimibe

Ezetimibe NEW

Price $41 $56 $70
Package 10mg 25mg 50mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Ezetimibe CAS No.: 163222-33-1
Purity: 99.97% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameEzetimibe
DescriptionEzetimibe (SCH 58235) is a dietary cholesterol absorption inhibitor that exerts its physiologic effect by decreasing cholesterol absorption.
Cell ResearchEzetimibe is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. Huh7 human hepatocytes are cultured in high glucose DMEM containing 10% FBS, 100 units/mL penicillin and 100 μg/mL streptomycin at 37°C in a 95% air/5% CO2 atmosphere. Hepatocytes are treated with or without Ezetimibe (10 μM, 1 h) and incubated with palmitic acid (PA, 0.5 mM, 24 h)[2].
Kinase AssayGST-p62 is prepared from Escherichia coli and 0.5 μg of the purified GST-p62 protein is used for in vitro AMPK phosphorylation assay. Phosphorylation of p62 protein by AMPK is determined by non-radioisotope method using γS-ATP. AMPK complex is immuno-purified from the HEK293 cells, to which either myc-AMPKα1 wild-type (WT) or myc-AMPKα1 kinase-dead mutant (KD, D157A) is transfected with Flag-AMPKβ1 and HA-AMPKγ1. AMPK complex is added into the reaction mixture containing 20 mM HEPES, pH7.4, 1 mM EGTA, 0.4 mM EDTA, 5 mM MgCl2, 0.05 mM DTT, 0.5 μg GST-p62, 0.2 mM AMP, and 1 mM ATPγS. Reaction is carried out at 37°C for 30 min, and then terminated by adding 20 mM EDTA. To detect γS-labeled p62 protein, the reaction product is alkylated with 2.5 mM PNBM for 2 h at room temperature and analyzed the products by western blotting using anti-thiophosphate antibody[1].
In vitroEzetimibe effectively inhibits the transport of cholesterol across the intestinal wall, thereby reducing plasma cholesterol in preclinical animal models of hypercholesterolemia. It eliminates exocrine pancreatic function in rats while maintaining bile flow. In hamsters fed with cholesterol, ezetimibe reduces plasma cholesterol and hepatic cholesterol accumulation, with an effective dose (ED50) of 0.04 mg/kg. It also decreases the surface area of aortic atherosclerotic lesions, from 20.2% in the control group to 4.1% in the group on a Western diet and 7.0% in mice on a low-fat cholesterol diet. Furthermore, ezetimibe reduces the cross-sectional area of carotid atherosclerotic lesions by 97% in the Western low-fat cholesterol diet group and by 91% in cholesterol-free mice.
In vivoEzetimibe significantly reduces the expression of mRNA for scavenger receptor class B type I (SR-BI), Niemann-Pick C1-like 1 protein (NPC1L1), ATP-binding cassette transporters, sub-family A member (ABCA), the β subunit of liver X receptor (LXRβ), retinoid X receptor γ (RXRγ), and steroid regulatory element-binding proteins 1 and 2 (SREBP-1 and -2). Ezetimibe notably decreases total cholesterol, low-density lipoprotein (LDL) cholesterol, and triglycerides, while moderately increasing high-density lipoprotein (HDL) cholesterol levels. In Caco-2 cells, Ezetimibe reduces cholesterol transport by 31% without affecting retinol transport.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 60 mg/mL (146.55 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 75 mg/mL (183.2 mM)
KeywordsSCH58235 | Autophagy | inhibit | Keap1-Nrf2 | Inhibitor | SCH-58235 | Ezetimibe
Inhibitors RelatedStavudine | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Paeonol | Naringin | Gefitinib
Related Compound LibrariesBioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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  • Since: 2011-01-07
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