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Torcetrapib CETP inhibitor

Cat.No.S2792

Torcetrapib (CP-529414) is a CETP inhibitor with IC50 of 37 nM, elevates HDL-C and reduces nonHDL-C in plasma. Phase 3.
Torcetrapib CETP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 600.47

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Chemical Information, Storage & Stability

Molecular Weight 600.47 Formula

C26H25F9N2O4

 Storage (From the date of receipt)
CAS No. 262352-17-0 Download SDF Storage of Stock Solutions

Synonyms CP-529414 Smiles CCC1CC(C2=C(N1C(=O)OCC)C=CC(=C2)C(F)(F)F)N(CC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)C(=O)OC

Solubility

In vitro
Batch:

DMSO : 120 mg/mL ( (199.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

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In vivo
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Mechanism of Action

Targets/IC50/Ki
CETP [1]
37 nM
In vitro
Torcetrapib dose-dependently increases aldosterone release from H295R cells after either 24 or 48 h of treatment with an EC50 of approximately 80 nM, this effect is mediated by calcium channel as calcium channel blockers completely blocks this compound-induced corticoid release and calcium increase. This chemical (1 μM) significantly increases the expression of steroidogenic gene, CYP11B2 and CYP11B1, in H295R cell lines. [2]
In vivo
Torcetrapib (< 100 mg, daily) changes the plasma distribution of CETP, as the apparent molecular weight of the CETP has shifted to a larger form, by 2 hours after the dose in healthy young subjects. This compound treatment with 10 mg, 30 mg, 60 mg, and 120 mg daily and 120 mg twice daily results in 16%, 28%, 62%, 73%, and 91% increases in plasma HDL-C, respectively, with no significant changes in TPC in healthy young subjects. [1] It results in an increase of 72.1% in high-density lipoprotein cholesterol and a decrease of 24.9% in low-density lipoprotein cholesterol, in addition to an increase of 5.4 mm Hg in systolic blood pressure, a decrease in serum potassium, and increases in serum sodium, bicarbonate, and aldosterone, in patients at high cardiovascular risk after 12 months' treatment. [3] This agent increases HDL cholesterol levels by 50% and 60% at dose of 60 mg daily and 120 mg daily, respectively, in both healthy and moderately hyperlipidemic subjects. It 60 mg daily increases HDL-mediated net cholesterol efflux from foam cells primarily by increasing HDL concentrations, whereas 120 mg daily of this compound increases cholesterol efflux both by increasing HDL concentration and by causing increased efflux at matched HDL concentrations. [4] This chemical (90 mg/kg/day) results in a 70% inhibition of CE transfer in rabbits fed an atherogenic diet. It (90 mg/kg/day) increases mean HDL-C levels by above 3-fold and apoA-I levels by 2.5-fold in plasma in rabbits fed an atherogenic diet. The treated animal has a multiple-fold increase in HDL-C AUC and a corresponding reduction in aortic lesion area with 60% reduction of aortic free cholesterol (FC) and cholesteryl ester (EC) in rabbits fed an atherogenic diet. Sera from this compound-treated rabbits stimulate free cholesterol efflux to a significantly greater extent than does sera from control rabbits. [5]
References
  • https://pubmed.ncbi.nlm.nih.gov/17322101/
  • https://pubmed.ncbi.nlm.nih.gov/17325387/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00139061 Completed
Hyperlipidemia
Pfizer
 March 2005 Phase 3

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