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Anacetrapib

Cat. No. M2142

Anacetrapib Structure

Synonym: MK-0859

Size Price Availability Quantity
10mg USD 290 In stock
50mg USD 990 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 637.51
Formula C30H25F10NO3
CAS Number 875446-37-0
Purity >99%
Solubility DMSO 100 mg/mL
Ethanol 100 mg/mL
Storage at -20°C
References

Biochemical characterization of cholesteryl ester transfer protein inhibitors.
Ranalletta M, et al. J Lipid Res. 2010 Sep;51(9):2739-52. PMID: 20458119.

Single-dose pharmacokinetics and pharmacodynamics of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.
Krishna R, et al. Br J Clin Pharmacol. 2009 Oct;68(4):535-45. PMID: 19843057.

Related CETP Products
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.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Anacetrapib, MK-0859 supplier, CETP, inhibitors

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