Anacetrapib (codenamed MK-0859) is a potent cholesteryl ester transfer protein (CETP) inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. Anacetrapib binds reversibly and dalcetrapib covalently to CETP. Anacetrapib inhibited CETP-mediated cholesteryl ester and triglyceride transfer with similar potencies. Anacetrapib potently blocks CE and TG transfer in 95% human serum. Single doses of anacetrapib markedly and dose-dependently inhibited serum CETP activity with peak effects of approximately 90% inhibition at t(max) and approximately 58% inhibition at 24 h post-dose. In addition, Anacetrapib promotes reverse cholesterol transport from macrophages, and leads to a 30% increase in fecal cholesterol content.
| Molecular Weight | 637.51 |
| Formula | C30H25F10NO3 |
| CAS Number | 875446-37-0 |
| Solubility (25°C) | DMSO 100 mg/mL Ethanol 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related CETP Products |
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| Obicetrapib
Obicetrapib 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. |
| Evacetrapib
Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP which inhibited human recombinant CETP protein (5.5 nM IC(50)) and CETP activity in human plasma (36 nM IC(50)) in vitro. |
| 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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