Torcetrapib

Torcetrapib (CP-529414) is a potent cholesteryl ester transfer protein (CETP) inhibitor with IC50 of 37 nM; shows the potential to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease.Atherosclerosis Phase 2 Discontinued (In Vitro) :The IC50 for Torcetrapib determined from the linear portion of the curves (25 to 80 nM) is 52 and 65 nM for the 3H-HDL and 14C-LDL cholesteryl ester transfer assays, respectively, using the specific activity-adjusted calculation, and 47 and 61 nM using a single exponential decay function.Torcetrapib (0, 0.5, 1, 5, and 10 μM) significantly reduced MCF-7 cells growth.Torcetrapib (0, 1, 5, 10, and 20 μM) does not inducing MCF-7 cells apoptosis.Torcetrapib (10 μM) binds to CETP with high affinity and down-regulates CETP expression. (In Vivo) :Torcetrapib (3, 10, or 30 mg/kg every day [qd]; oral gavage for 14 days) significantly increases high-density lipoprotein (HDL) cholesterol and reduceslow-density lipoprotein (LDL) cholesterol, and there is a tendency for Torcetrapib to reduce very-low-density lipoprotein (VLDL) cholesterol and triglycerides. Maximal increase in HDL cholesterol is 53% with Torcetrapib.

262352-17-0

CP-529414

>98% (HPLC)

10 mM in DMSO

O=C (N1[C@H] (CC) C[C@H] (N (CC2=CC (C (F) (F) F) =CC (C (F) (F) F) =C2) C (OC) =O) C3=C1C=CC (C (F) (F) F) =C3) OCC

C26H25F9N2O4

600.4733

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.