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 properties.
IC50&Target
CETP
体外研究
CP-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.
体内研究
CP-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.
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.
分子式
C27H27F9N2O3
分子量
598.50
CAS号
261947-38-0
运输条件
Room temperature in continental US; may vary elsewhere.