Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Purity: ≥98%
Evacetrapib (also known as LY-2484595; LY2484595), a benzazepine compound, is a potent and selective inhibitor of CETP (Cholesteryl ester transfer protein) with the potential to lower cholesterol levels and to prevent cardiovascular diseases. It inhibits CETP with an IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Evacetrapib inhibits cholesterylester transfer protein, which transfers and thereby increases high-density lipoprotein and lowers low-density lipoprotein. It is thought that modifying lipoprotein levels modifies the risk of cardiovascular disease.
ln Vitro |
The new CETP inhibitor evetrapib is based on benzazepine. Absolute potency of the drug in the buffer CETP assay is 5.5 nM. As for the human plasma CETP assay, the recombinant protein or CETP from human plasma have a CETP concentration of roughly 2 μg/mL (25 nM), and the 36 nM IC50 value confirms that ezetapanib is a strong CETP inhibitor. According to some reports, evacetrapib is far more effective than dalecapib [1].
|
||
---|---|---|---|
ln Vivo |
Evacetrapib displays a considerable increase in HDL cholesterol and an ex vivo CETP inhibition ED50 of less than 5 mg/kg at 8 hours post oral dosing in double transgenic mice expressing human CETP and apoAI. Crucially, when rats given high exposure multiples of ezetimibe are compared to the positive control, torcetrapib, there is no rise in blood pressure. When taken orally, ezetimibe at a dose of 30 mg/kg inhibits CETP activity by 98.4%, 98.6%, and 18.4% at 4, 8, and 24 hours after the dose, respectively. Eight hours after oral delivery, a 129.7% increase in HDL-C was observed when ezetimib was dosed at 30 mg/kg[1].
|
||
Animal Protocol |
|
||
References |
[1]. Cao G, et al. Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure. J Lipid Res. 2011 Dec;52(12):2169-76
|
Molecular Formula |
C31H36F6N6O2
|
|
---|---|---|
Molecular Weight |
638.65
|
|
CAS # |
1186486-62-3
|
|
Related CAS # |
|
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
|
SMILES |
FC(C1C([H])=C(C(F)(F)F)C([H])=C(C=1[H])C([H])([H])N(C1N=NN(C([H])([H])[H])N=1)[C@]1([H])C2=C([H])C(C([H])([H])[H])=C([H])C(C([H])([H])[H])=C2N(C([H])([H])C([H])([H])C1([H])[H])C([H])([H])C1([H])C([H])([H])C([H])([H])C([H])(C(=O)O[H])C([H])([H])C1([H])[H])(F)F
|
|
Synonyms |
|
|
HS Tariff Code |
2934.99.9001
|
|
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)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.91 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 25.0 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: ≥ 2.5 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 15% Captisol: 30 mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.5658 mL | 7.8290 mL | 15.6580 mL | |
5 mM | 0.3132 mL | 1.5658 mL | 3.1316 mL | |
10 mM | 0.1566 mL | 0.7829 mL | 1.5658 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02226653 | Completed Has Results | Drug: Evacetrapib | Healthy Volunteers | Eli Lilly and Company | September 2014 | Phase 1 |
NCT01903434 | Completed Has Results | Drug: Evacetrapib | Healthy Volunteers | Eli Lilly and Company | July 2013 | Phase 1 |
NCT01825889 | Completed Has Results | Drug: Evacetrapib | Cardiovascular Disease | Eli Lilly and Company | April 2013 | Phase 1 |
NCT02497391 | Completed Has Results | Drug: Evacetrapib | Healthy | Eli Lilly and Company | July 2015 | Phase 1 |