Torcetrapib

SKU: orb1225479

Description

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.

Key Properties

• CAS Number: 262352-17-0
• MW: 600.4733
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₅F₉N₂O₄
• SMILES: 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
• Target: CETP
• Solubility: 10 mM in DMSO

Bioactivity

• 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. 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.
• 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CP-529414

Quick Database Links

Gene Symbol

CETP