Trandolapril
Based on 1 Customer Validation
Trandolapril (RU44570) is a nonsulfhydryl proagent that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI).
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- Pureté: 99.88%
- CAS No.: 87679-37-6
- Formule: C24H34N2O5
- Masse moléculaire:430.54
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Target: Angiotensin-converting Enzyme (ACE)[1]
Trandolapril (0.02 mM, 1 mM; 3 d) inhibits cell growth and induces cell apoptosis, increases the percentage of apoptotic cells in K562 cell line[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562, KU812, U937 and HL60
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Concentration:0-2 mM
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Incubation Time:0, 1, 2, 3 days
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Result:Inhibited K562, KU812, U937 at 1 mM and inhibited HL60 at 0.02 mM.
Trandolapril (0.3 mg/kg/day; p.o.; 4 weeks) improves arterial mechanics in rats, prevents arterial hypertrophy, collagen and cellular fibronectin accumulation[3].
randolapril (0.3 mg/kg/day; p.o.; 4 months) exhibits a chronic anti-hypertension effects in rats, results in blood pressure decreasing[3].
Trandolapril (0.25 mg/kg; p.o.; twice a day; 4 months) inhibits Atherosclerosis in the Watanabe Heritable Hyperlipidemic Rabbit[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:UUD (unilateral ureteral obstruction) model in Male CD-1 mice (18-22 g)[2]
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Dosage:3 mg/kg
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Administration:Oral gavage; daily, for 7 days
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Result:Resulted in renal interstitial matrix expression (including fibronectin, type I, and type III collagen) decreasing, and inhibited myofibroblast activation by surprising a-smooth muscle actin (a-SMA) expression, decreased the RANTES (regulated on activation, normal T cell expressed and secreted) and TNF-α level.
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Animal Model:SHR model (spontaneously hypertensive rats, 4-week-old)[3]
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Dosage:0.3 mg/kg
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Administration:Oral gavage; daily for 4 weeks
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Result:Reduced collagen content in the aortic media and increased ariterial distensibility up to about 80%.
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Animal Model:Watanabe heritable hyperlipidemic rabbit (3 months old)[4]
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Dosage:0.25 mg/kg
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Administration:Oral gavage; twice a day; 9 months
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Result:Decreased in atherosclerotic involvement of the intimal surface, and also decreased cholesterol content in descending thoracic aorta.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 87679-37-6
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Appearance Solid
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Masse moléculaire 430.54
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Formule C24H34N2O5
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Color White to off-white
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SMILES
O=C([C@H]1N(C([C@@H](N[C@H](C(OCC)=O)CCC2=CC=CC=C2)C)=O)[C@@]3([H])CCCC[C@]3([H])C1)O
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Synonyms
RU44570
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (232.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Peters DC, et al. Trandolapril. An update of its pharmacology and therapeutic use in cardiovascular disorders. Drugs. 1998 Nov;56(5):871-93. [Content Brief]
[2]. Tan X, et al. Combination therapy with paricalcitol and trandolapril reduces renal fibrosis in obstructive nephropathy. Kidney Int. 2009 Dec;76(12):1248-57. [Content Brief]
[3]. Koffi I, et al. Prevention of arterial structural alterations with verapamil and trandolapril and consequences for mechanical properties in spontaneously hypertensive rats. Eur J Pharmacol. 1998 Nov 13;361(1):51-60. [Content Brief]
[4]. Chobanian AV, et al. Trandolapril inhibits atherosclerosis in the Watanabe heritable hyperlipidemic rabbit. Hypertension. 1992 Oct;20(4):473-7. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3227 mL | 11.6133 mL | 23.2266 mL | 58.0666 mL |
| 5 mM | 0.4645 mL | 2.3227 mL | 4.6453 mL | 11.6133 mL | |
| 10 mM | 0.2323 mL | 1.1613 mL | 2.3227 mL | 5.8067 mL | |
| 15 mM | 0.1548 mL | 0.7742 mL | 1.5484 mL | 3.8711 mL | |
| 20 mM | 0.1161 mL | 0.5807 mL | 1.1613 mL | 2.9033 mL | |
| 25 mM | 0.0929 mL | 0.4645 mL | 0.9291 mL | 2.3227 mL | |
| 30 mM | 0.0774 mL | 0.3871 mL | 0.7742 mL | 1.9356 mL | |
| 40 mM | 0.0581 mL | 0.2903 mL | 0.5807 mL | 1.4517 mL | |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4645 mL | 1.1613 mL | |
| 60 mM | 0.0387 mL | 0.1936 mL | 0.3871 mL | 0.9678 mL | |
| 80 mM | 0.0290 mL | 0.1452 mL | 0.2903 mL | 0.7258 mL | |
| 100 mM | 0.0232 mL | 0.1161 mL | 0.2323 mL | 0.5807 mL |
Trandolapril Related Classifications
HY-B0592 Related Classifications
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- Trandolapril
- 87679-37-6
- RU44570
- RU 44570
- RU-44570
- Angiotensin-converting Enzyme (ACE)
- congestive heart failure
- CHF
- myocardial infarction
- MI
- Trandolaprilat
- orally active
- hypertension
- nonsulfhydryl
- arterial hypertrophy
- collagen
- cellular fibronectin accumulation
- spontaneously hypertensive rats
- UUD model
- unilateral ureteral obstruction
- UUO model
- Inhibitor
- inhibitor
- inhibit