Torcetrapib
Torcetrapib
CAS: 262352-17-0
Molecular Formula: C26H25F9N2O4
Torcetrapib - Names and Identifiers
Torcetrapib - Physico-chemical Properties
| Molecular Formula | C26H25F9N2O4 |
| Molar Mass | 600.47 |
| Density | 1.42 |
| Melting Point | 54-58°C |
| Boling Point | 504.8±50.0 °C(Predicted) |
| Solubility | Soluble in chloroform, methanol, ethanol (~10 mg/ml), DMSO (120 mg/ml at 25 °C), DMF (~20 mg/ml), and water (<1 mg/ml at 25 °C). |
| Appearance | powder |
| Color | white |
| pKa | -1.87±0.40(Predicted) |
| Storage Condition | Store at RT |
| MDL | MFCD09260777 |
| Use | Torcetrapib is a CETP inhibitor with IC50 of 37 nM, which increases HDL-C in plasma and reduces nonHDL-C. Phase 3. |
| In vitro study | Treatment of H295R cells with Torcetrapib for 24 or 48 hours showed a dose-dependent increase in aldosterone release by Torcetrapib with an EC50 of approximately 80 nM. This effect can be modulated by calcium channels, as calcium channel blockers can completely block the torcetrapib-induced release of adrenocortical lipools and the increase in calcium. In the H295R cell line, Torcetrapib (1 μm) significantly increased the expression of the steroid-producing genes, CYP11B2 and CYP11B1. |
| In vivo study | Torcetrapib (< 100 mg per day) changed the plasma distribution of CETP after 2 hours in the young healthy group because the apparent molecular weight of CETP migrated to a larger form. In the young healthy group, 10 mg, 30 mg, 60 mg and 120 mg daily and 120 mg Torcetrapib twice daily increased plasma levels by HDL-C, respectively, by 16%, 28, 62, 73% and 91% while TPC did not change significantly. In patients at high risk of cardiovascular disease, Torcetrapib treatment for 12 hours resulted in a 72.1% increase in HDL cholesterol and a 24.9% decrease in LDL cholesterol, a 5.4mm increase in systolic blood pressure and a decrease in serum potassium concentration, serum sodium concentration, bicarbonate concentration and aldosterone concentration increased. Torcetrapib 60mg per day and 50% mg per day increased HDL cholesterol levels by 60% and in the healthy and moderately hyperlipidaemic groups, respectively. Torcetrapib 60mg per day increased HDL-mediated net cholesterol efflux from foam cells, mainly due to increased HDL concentration, while 120mg per day increased net cholesterol efflux, I .e., due to increased HDL concentration, also due to the increased efflux at the matched HDL concentration. In rabbits fed the Atherogenic diet, Torcetrapib (90 mg/kg/day) inhibited CE metastasis by 70% and increased plasma levels by an average of HDL-C by a factor of 3, increased the level apoA-I by a factor of 2.5. Torcetrapib treatment in rabbits fed the Atherogenic diet resulted in a multiple increase in HDL-C AUC levels with a decrease in aortic lesion area, in addition to a 60% decrease in aortic free cholesterol (FC) and cholesterol ester (EC). Torcetrapib treated rabbits significantly stimulated free cholesterol efflux compared to serum. |
Torcetrapib - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| WGK Germany | 3 |
Torcetrapib - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.665 ml | 8.327 ml | 16.654 ml |
| 5 mM | 0.333 ml | 1.665 ml | 3.331 ml |
| 10 mM | 0.167 ml | 0.833 ml | 1.665 ml |
| 5 mM | 0.033 ml | 0.167 ml | 0.333 ml |
Last Update：2024-01-02 23:10:35
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CAS: 262352-17-0
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