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Evacetrapib (investigational name LY2484595) is a potent and selective inhibitor of CETP both in vitro and in vivo. Evacetrapib inhibits cholesterylester transfer protein, which transfers and thereby increases high-density lipoprotein and lowers low-density lipoprotein. In double transgenic mice expressing human CETP and apoAI, evacetrapib exhibited an ex vivo CETP inhibition ED(50) of less than 5 mg/kg at 8 h post oral dose and significantly elevated HDL cholesterol. In addition, in a human adrenal cortical carcinoma cell line (H295R cells), evacetrapib did not induce aldosterone or cortisol biosynthesis whereas torcetrapib dramatically induced aldosterone and cortisol biosynthesis.
| Molecular Weight | 638.65 |
| Formula | C31H36F6N6O2 |
| CAS Number | 1186486-62-3 |
| Solubility (25°C) | DMSO 14 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CETP Products |
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| Obicetrapib
Obicetrapib (DEZ-001) is a selective, orally active cholesterol transporter protein (CETP) inhibitor that blocks the function of CETP and significantly reduces LDL-C while significantly increasing HDL-C levels, and may be used in studies related to atherosclerosis and Alzheimer's disease (AD). |
| Dalcetrapib
Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. |
| Anacetrapib
Anacetrapib is an orally active and potent inhibitor of CETP with IC50 of 7.9 nM and 11.8 nM for rhCETP and mutant CETP(C13S) respectively. |
| Torcetrapib
Torcetrapib (CP-529414) is a prototype cholesteryl ester transfer protein (CETP) inhibitor with potential for decreasing atherosclerotic disease, increased cardiovascular events in clinical trials. |
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