トルセトラピブ
Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.82%
- CAS 番号: 262352-17-0
- 分子式: C26H25F9N2O4
- 分子量:600.47
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Metabolism/Protease Compound Library
HY-L012
-
Clinical Compound Library
HY-L026
-
Drug Repurposing Compound Library
HY-L035
-
Endocrinology Compound Library
HY-L047
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Lipid Metabolism Compound Library
HY-L091
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
生物活性
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF-7 cells
-
Concentration:0, 0.5, 1, 5, and 10 μM
-
Incubation Time:5 days
-
Result:Significantly reduced cell growth.
-
Cell Line:MCF-7 cells
-
Concentration:10 μM
-
Incubation Time:48 hours
-
Result:Down-regulated CETP mRNA expression.
MedChemExpress (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.
化学情報
-
CAS 番号 262352-17-0
-
性状 Solid
-
分子量 600.47
-
分子式 C26H25F9N2O4
-
Color White to off-white
-
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
-
別名
Torcetrapib; CP-529414
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (166.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
-
データシート (277 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6654 mL | 8.3268 mL | 16.6536 mL | 41.6341 mL |
| 5 mM | 0.3331 mL | 1.6654 mL | 3.3307 mL | 8.3268 mL | |
| 10 mM | 0.1665 mL | 0.8327 mL | 1.6654 mL | 4.1634 mL | |
| 15 mM | 0.1110 mL | 0.5551 mL | 1.1102 mL | 2.7756 mL | |
| 20 mM | 0.0833 mL | 0.4163 mL | 0.8327 mL | 2.0817 mL | |
| 25 mM | 0.0666 mL | 0.3331 mL | 0.6661 mL | 1.6654 mL | |
| 30 mM | 0.0555 mL | 0.2776 mL | 0.5551 mL | 1.3878 mL | |
| 40 mM | 0.0416 mL | 0.2082 mL | 0.4163 mL | 1.0409 mL | |
| 50 mM | 0.0333 mL | 0.1665 mL | 0.3331 mL | 0.8327 mL | |
| 60 mM | 0.0278 mL | 0.1388 mL | 0.2776 mL | 0.6939 mL | |
| 80 mM | 0.0208 mL | 0.1041 mL | 0.2082 mL | 0.5204 mL | |
| 100 mM | 0.0167 mL | 0.0833 mL | 0.1665 mL | 0.4163 mL |
Torcetrapib 関連分類
HY-12089 関連分類
Powered by Bioz