1. Metabolic Enzyme/Protease
  2. CETP
  3. Torcetrapib

Torcetrapib (Synonyms: CP-529414)

Cat. No.: HY-12089 Purity: 99.39%
Handling Instructions

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.

For research use only. We do not sell to patients.

Torcetrapib Chemical Structure

Torcetrapib Chemical Structure

CAS No. : 262352-17-0

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 140 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 140 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 106 In-stock
Estimated Time of Arrival: December 31
10 mg USD 131 In-stock
Estimated Time of Arrival: December 31
50 mg USD 499 In-stock
Estimated Time of Arrival: December 31
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Description

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[1].

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[1].
Torcetrapib (0, 0.5, 1, 5, and 10 μM) significantly reduced MCF-7 cells growth[2].
Torcetrapib (0, 1, 5, 10, and 20 μM) does not inducing MCF-7 cells apoptosis[2].
Torcetrapib (10 μM) binds to CETP with high affinity and down-regulates CETP expression[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Tg (B6; SJL-TgN (CETP)-TgN (ApoB100)) mice at 6 to 7 weeks of age[3]
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.
Molecular Weight

600.47

Formula

C26H25F9N2O4

CAS No.
SMILES

O=C(N1[[email protected]](CC)C[[email protected]](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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (166.54 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6654 mL 8.3268 mL 16.6536 mL
5 mM 0.3331 mL 1.6654 mL 3.3307 mL
10 mM 0.1665 mL 0.8327 mL 1.6654 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.16 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.16 mM); Clear solution

*All of the co-solvents are available by MCE.
References
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Torcetrapib
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