Size | Price | Stock | Qty |
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2mg |
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5mg |
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10mg |
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Other Sizes |
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Ezetimibe (SCH58235; SCH-58235; Zetia, Ezetrol) is a selective inhibitor of cholesterol absorption in the gut used to lower cholesterol levels. Ezetimibe ketone is a phase-I metabolite of ezetimibe.
Targets |
NPC1L1; Nrf2
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References |
[1]. Efficient and scalable process for the synthesis of antihypercholesterolemic drug ezetimibe. Synthetic Communications. 2016, 46:20, 1687-1693.
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Molecular Formula |
C24H19NO3
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Molecular Weight |
407.40936
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Exact Mass |
407.13
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Elemental Analysis |
C, 70.75; H, 4.70; F, 9.33; N, 3.44; O, 11.78
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CAS # |
191330-56-0
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Related CAS # |
191330-56-0
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Appearance |
Solid powder
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SMILES |
C1=CC(=CC=C1[C@@H]2[C@H](C(=O)N2C3=CC=C(C=C3)F)CCC(=O)C4=CC=C(C=C4)F)O
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InChi Key |
UEPZDXMEEKCJSP-FYYLOGMGSA-N
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InChi Code |
InChI=1S/C24H19F2NO3/c25-17-5-1-15(2-6-17)22(29)14-13-21-23(16-3-11-20(28)12-4-16)27(24(21)30)19-9-7-18(26)8-10-19/h1-12,21,23,28H,13-14H2/t21-,23-/m1/s1
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Chemical Name |
(3R,4S)-1-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-oxopropyl]-4-(4-hydroxyphenyl)azetidin-2-one
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Synonyms |
Ezetimibe ketone; EZM K; EZM-K
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~245.5 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.25 mg/mL (3.07 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4545 mL | 12.2726 mL | 24.5453 mL | |
5 mM | 0.4909 mL | 2.4545 mL | 4.9091 mL | |
10 mM | 0.2455 mL | 1.2273 mL | 2.4545 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Ezetimibe improves hepatic steatosis in OLETF rats. World J Gastroenterol . 2015 Jul 7;21(25):7754-63. td> |
Ezetimibe increases autophagy makers in OLETF liver tissue. World J Gastroenterol . 2015 Jul 7;21(25):7754-63. td> |
Ezetimibe treatment attenuates triglycerides accumulation and induces autophagy in hepatocytes. World J Gastroenterol . 2015 Jul 7;21(25):7754-63. td> |
Ezetimibe increases autophagosome formation and autophagic flux in hepatocytes. World J Gastroenterol . 2015 Jul 7;21(25):7754-63. td> |