CP-532623 (C09-1120-228)

CP-532623 is a CETP inhibitor and elevates high-density lipoprotein cholesterolion. CP-532623 is a close structural analogue of Torcetrapib. CP-532623 has highly lipophilic propertiesIn VitroCP-532623 is highly lymphatically transported (28% of dose), and lymphatic transport is closely correlated with drug affinity for ex-vivo lymph lipoproteins or triglyceride emulsions and poorly relates to solubility in mixtures of lipoprotein core and/or surface lipids. CP-532623 alters the kinetics of lymph lipid transport and decreases lymph lipid transport in chylomicrons. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoCP-532623 (50 mg; oral administration; adult male greyhound dogs) treatment substantially transports into the lymphatic system (>25% dose) in fed and fasted dogs. Food enhances oral bioavailability (from 44 to 58%, respectively) and the proportion of the absorbed dose transports via the lymph (from 61 to 86% and from 68 to 83%, respectively). Lymphatic triglyceride transport is significantly lower in fed dogs administered CP-532623. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult male greyhound dogs (27-39 kg)Dosage: 50 mg Administration: Oral administration with a long-chain lipid formulation to fed lymphcannulated Result: Substantially transported into the lymphatic system (>25% dose) in fed and fasted dogs. Food enhanced oral bioavailability and the proportion of the absorbed dose transported via the lymph.Form:SolidIC50& Target:CETP. Molecular Formula: C27H27F9N2O3 Molecular Weight: 598.5 PubChem CID: 10145345 Isomeric SMILES: CC[C@@H]1C[C@@H](C2=C(N1C(=O)OC(C)C)C=CC(=C2)C(F)(F)F)N(CC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)C(=O)C