[CAS NO. 262352-17-0] Torcetrapib
PRODUCTS SPECIFICATIONS [262352-17-0]
DESCRIPTION [262352-17-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 600.47 |
| Molecular 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 |
Summary
In Vitro
The IC
50
for Torcetrapib determined from the linear portion of the curves (25 to 80 nM) is 52 and 65 nM for the
3
H-HDL and
14
C-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. |
Appearance
Solid
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
DMSO : ≥ 100 mg/mL ( 166.54 mM )
* "≥" means soluble, but saturation unknown.
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 |
References
- [1] Ronald W Clark, et al. Raising high-density lipoprotein in humans through inhibition of cholesteryl ester transfer protein: an initial multidose study of torcetrapib.Arterioscler Thromb Vasc Biol. 2004 Mar;24(3):490-7.
- [2] Luke Esau, et al. Identification of as a molecular target for estrogen positive breast cancer cell death by cholesterol depleting agents. Genes Cancer. 2016 Sep;7(9-10):309-322.
- [3] Michael K Hansen,et al. Selective CETP inhibition and PPARalpha agonism increase HDL cholesterol and reduce LDL cholesterol in human ApoB100/human CETP transgenic mice.J Cardiovasc Pharmacol Ther. 2010 Jun;15(2):196-202.
Synonyms