| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. Cell Viability Assay Cell Line: | ||||||||||||
| 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]. Animal Model: | ||||||||||||
| Name | Torcetrapib | ||||||||||||
| CAS | 262352-17-0 | ||||||||||||
| Formula | C26H25F9N2O4 | ||||||||||||
| Molar Mass | 600.47 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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 CETP 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. |
Torcetrapib
CAS: 262352-17-0 F: C26H25F9N2O4 W: 600.47
Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition
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