包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
50mg | 电议 |
100mg | 电议 |
Cell lines | Caco-2 cell lines |
Preparation method | The solubility of this compound in DMSO is >20.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 1-10 μg/mL |
Applications | In Caco-2 cells, ezetimibe is an inhibitor of carotenoid transport, an effect that decreases with increasing polarity of the carotenoid molecule. Ezetimibe dose not only interact physically with cholesterol transporter, but also downregulate expression of these proteins. |
Animal models | apolipoprotein E knockout (apoE-/-) mice |
Dosage form | 5 mg/kg per day for 6 months |
Application | 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. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
产品描述 | Ezetimibe is a potent and novel inhibitor of cholesterol absorption [1]. Cholesterol is a lipid molecule and is required to build and maintain membranes structural integrity and fluidity. Also, it serves as a precursor of vitamin D, bile acids and steroid hormones. In differentiated Caco-2 cells incubated with a carotenoid (1 μM), ezetimibe (10 mg/L) inhibited carotenoid transport with 50% inhibition for ɑ-carotene and β-carotene. Also, it inhibited the transport of β-cryptoxanthin, lycopene and lutein:zeaxanthin(1:1). At the same time, ezetimibe inhibited cholesterol transport by 31%. Ezetimibe decreased the expression of the surface receptors SR-BI, ATP binding cassette transporter, subfamily A (ABCA1), Niemann-Pick type C1 Like 1 protein (NPC1L1) and retinoid acid receptor (RAR)γ, sterol-regulatory element binding proteins SREBP-1 and SREBP-2, and liver X receptor (LXR)β [3]. In apolipoprotein E knockout (apoE-/-) mice, ezetimibe (3 mg/kg) inhibited cholesterol absorption by 90%. Ezetimibe reduced plasma cholesterol, increased HDL levels, and inhibits the progression of atherosclerosis [1]. In phase III human trials, Ezetimibe (10 mg) significantly reduced the levels of LDL cholesterol, total cholesterol and triglycerides and increased the level of HDL cholesterol [2]. References: |