Torcetrapib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Torcetrapib (CP-529414) 是一种有效的胆固醇酯转移蛋白 (CETP) 抑制剂，IC50 为 37 nM。

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.

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. 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.

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 daysResult: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.

CP-529414

Metabolic Enzyme/Protease

CETP

CETP

Cardiovascular Disease

Atherosclerosis

262352-17-0

600.4733

C26H25F9N2O4

>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

1(2H)-Quinolinecarboxylic acid, 4-[[[3,5-bis(trifluoromethyl)phenyl]methyl](methoxycarbonyl)amino]-2-ethyl-3,4-dihydro-6-(trifluoromethyl)-, ethyl ester, (2R,4S)-

(-20℃)

With Ice Pack

≥ 2 years