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Ezetimibe
Cat No.
CEI-1335
Product Overview
Ezetimibe is a potent and novel inhibitor of cholesterol absorption. 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. 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 atherosclerosi. 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.
CAS No.
163222-33-1
Molecular Weight
409.4
Purity
0.9974
Storage
Store at-20°C
Targets
Cholesterol transport
Molecular Formula
C24H21F2NO3
Chemical Name
(3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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