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| 25mg |
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Purity: ≥98%
Torcetrapib (formerly CP 529414; CP-529,414; CP-529414) is a novel and potent CETP (Cholesteryl ester transfer protein) inhibitor with the potential to lower cholesterol levels and to treat cardiovascular diseases. It inhibits CETP with an IC50 of 37 nM. Torcetrapib is able to elevate plasma HDL-C and reducs non-HDL-C, and thus is being studied to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease.
| ln Vitro |
Using the specific activity-adjusted calculation, the IC50 for trocetrapib is 52 and 65 nM for the 3H-HDL and 14C-LDL cholesteryl ester transfer tests, respectively, and 47 and 61 nM using a single exponential decay function[1]. This information is derived from the linear region of the curves, which ranges from 25 to 80 nM. The proliferation of MCF-7 cells was dramatically inhibited by trocetrapib (0, 0.5, 1, 5, and 10 μM)[2]. Torcetrapib at concentrations of 0, 1, 5, 10, and 20 μM does not cause apoptosis in MCF-7 cells[2]. The high affinity binding of trocetrapib (10 μM) to CETP results in the downregulation of CETP expression[2].
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| ln Vivo |
Torcetrapib increases high-density lipoprotein (HDL) cholesterol and decreases low-density lipoprotein (LDL) cholesterol significantly (3, 10, or 30 mg/kg every day [qd]; oral gavage for 14 days). Additionally, there is a tendency for Torcetrapib to lower triglycerides and very-low-density lipoprotein (VLDL) cholesterol. With trocetapib, the maximum increase in HDL cholesterol is 53%[3].
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| Cell Assay |
Cell Viability Assay
Cell Types: MCF-7 cells Tested Concentrations: 0, 0.5, 1, 5, and 10 μM Incubation Duration: 5 days Experimental Results: Dramatically decreased cell growth. RT-PCR Cell Types: MCF-7 cells Tested Concentrations: 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: Down-regulated CETP mRNA expression. |
| Animal Protocol |
Animal/Disease Models: Male Tg (B6; SJL-TgN (CETP)-TgN (ApoB100)) mice at 6 to 7 weeks of age[3]
Doses: 3, 10, and 30 mg/kg Route of Administration: Orally every day for 14 days Experimental Results: Dramatically 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. Dramatically diminished LDL cholesterol by 44% and 35% at 10 and 30 mg/kg compared to baseline, respectively, after 14 days of treatment. |
| 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 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. |
| Molecular Formula |
C26H25F9N2O4
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| Molecular Weight |
600.47
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| CAS # |
262352-17-0
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| Related CAS # |
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| 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
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| InChi Key |
CMSGWTNRGKRWGS-NQIIRXRSSA-N
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| InChi Code |
InChI=1S/C26H25F9N2O4/c1-4-18-12-21(19-11-15(24(27,28)29)6-7-20(19)37(18)23(39)41-5-2)36(22(38)40-3)13-14-8-16(25(30,31)32)10-17(9-14)26(33,34)35/h6-11,18,21H,4-5,12-13H2,1-3H3/t18-,21+/m1/s1
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| Chemical Name |
ethyl (2R,4S)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-methoxycarbonylamino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinoline-1-carboxylate
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.16 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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