Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM.
体外研究
The IC50 for Torcetrapib determined from the linear portion of the curves (25 to 80 nM) is 52 and 65 nM for the H-HDL and C-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.
Cell Viability Assay
Cell Line:
MCF-7 cells
Concentration:
0, 0.5, 1, 5, and 10 μM
Incubation Time:
5 days
Result:
Significantly reduced cell growth.
RT-PCR
Cell Line:
MCF-7 cells
Concentration:
10 μM
Incubation Time:
48 hours
Result:
Down-regulated CETP mRNA expression.
体内研究
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.
Animal Model:
Male Tg (B6; SJL-TgN (CETP)-TgN (ApoB100)) mice at 6 to 7 weeks of age
Dosage:
3, 10, and 30 mg/kg
Administration:
Orally every day for 14 days
Result:
Significantly Increased HDL cholesterol by 27%, 24%, and 53% in the 3, 10, and 30 mg/kg groups compared to baseline, respectively, after 14 days of treatment.
Significantly decreased LDL cholesterol by 44% and 35% at 10 and 30 mg/kg compared to baseline, respectively, after 14 days of treatment.
分子式
C26H25N2O4F9
分子量
600.47
CAS号
262352-17-0
中文名称
托彻普;托斯瑞比
运输条件
Room temperature in continental US; may vary elsewhere.