Trandolaprilangiotensin-converting enzyme (ACE) inhibitor CAS# 87679-37-6 |
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Quality Control & MSDS
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| Cas No. | 87679-37-6 | SDF | Download SDF |
| PubChem ID | 5484727 | Appearance | Powder |
| Formula | C24H34N2O5 | M.Wt | 430.54 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 100 mg/mL (232.27 mM; Need ultrasonic) | ||
| Chemical Name | (2S,3aR,7aS)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid | ||
| SMILES | CCOC(=O)C(CCC1=CC=CC=C1)NC(C)C(=O)N2C3CCCCC3CC2C(=O)O | ||
| Standard InChIKey | VXFJYXUZANRPDJ-WTNASJBWSA-N | ||
| Standard InChI | InChI=1S/C24H34N2O5/c1-3-31-24(30)19(14-13-17-9-5-4-6-10-17)25-16(2)22(27)26-20-12-8-7-11-18(20)15-21(26)23(28)29/h4-6,9-10,16,18-21,25H,3,7-8,11-15H2,1-2H3,(H,28,29)/t16-,18+,19-,20-,21-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
Trandolapril Dilution Calculator
Trandolapril Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3227 mL | 11.6133 mL | 23.2266 mL | 46.4533 mL | 58.0666 mL |
| 5 mM | 0.4645 mL | 2.3227 mL | 4.6453 mL | 9.2907 mL | 11.6133 mL |
| 10 mM | 0.2323 mL | 1.1613 mL | 2.3227 mL | 4.6453 mL | 5.8067 mL |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4645 mL | 0.9291 mL | 1.1613 mL |
| 100 mM | 0.0232 mL | 0.1161 mL | 0.2323 mL | 0.4645 mL | 0.5807 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Correction: Effects of Verapamil SR and Atenolol on 24-Hour Blood Pressure and Heart Rate in Hypertension Patients with Coronary Artery Disease: An International Verapamil SR-Trandolapril Ambulatory Monitoring Substudy.[Pubmed:27258057]
PLoS One. 2016 Jun 3;11(6):e0157212.
[This corrects the article DOI: 10.1371/journal.pone.0122726.].
The effects of dual and triple combinations of trandolapril, telmisartan, and verapamil on overt proteinuria in the patients with diabetic nephropathy.[Pubmed:27215243]
Saudi J Kidney Dis Transpl. 2016 May;27(3):512-8.
Diabetic nephropathy (DN) is one of the most important causes of the end-stage renal failure and its prevalence is found to be increasing. The presence of hypertension and progressive proteinuria is among the important findings. In this study, the effects of double and triple combinations of Trandolapril, telmisartan, and verapamil on proteinuria were investigated in diabetic patients with nephropathy. Seventy-eight patients (mean age: 56.11 +/- 11.26 years; 47 females and 31 males) with overt proteinuria and DN were included in this study. The patients were divided into four groups: Group I (n: 18, Trandolapril + telmisartan), Group II (n: 20, Trandolapril + verapamil), Group III (n: 20, Trandolapril +telmisartan + verapamil), and Group IV (n: 20, telmisartan + verapamil). At the end of a three-month therapy, within and between group comparisons were done about the effects of the use of double or triple drug combinations on proteinuria, glomerular filtration rate (GFR), electrolytes, serum albumin, low-density lipoprotein (LDL)- cholesterol, and HbA1C. There was no significant difference among groups in terms of age, gender, diabetes duration, body mass index, and retinopathy frequency. The decreases in proteinuria and mean arterial blood pressure (MABP) were significant in all groups. The decrease in proteinuria was independent of the decrease in MABP [the reduction rate in proteinuria was 39% (P <0.001) in Group I, 37% (P <0.001) in Group II, 42% (P <0.001) in Group III, and 43% (P <0.001) in Group IV; the reduction rate in MABP was 10.6% (P <0.001) in Group I, 13.7% (P <0.001) in Group II, 17.5% (P <0.001) in Group III, and 15.4% (P <0.001) in Group IV]. Decrease in HbA1C (before and after treatment) was significant in Groups III and IV when com- pared to Groups I and II. Any adverse event, like hyperkalemia, was not observed. There was no significant difference among the groups in terms of GFR, LDL-cholesterol, albumin, and potassium. All the patients tolerated the drugs well. In conclusion, in patients with DN, both double or triple combinations of Trandolapril, telmisartan and verapamil resulted in significant decreases in proteinuria and MABP. Triple combinations did not have any superiority over double combinations. Therefore, the suitable drug combinations may be chosen according to the clinical status of a patient.
Long-Term Mortality in Hypertensive Patients With Coronary Artery Disease: Results From the US Cohort of the International Verapamil (SR)/Trandolapril Study.[Pubmed:27620390]
Hypertension. 2016 Nov;68(5):1110-1114.
The dyad of hypertension and coronary artery disease is prevalent; however, data on systolic blood pressure (SBP) control and long-term all-cause mortality are lacking. Using extended follow-up data from the US cohort of the International Verapamil (SR)/Trandolapril Study (mean 11.6 years), subjects were categorized by age at enrollment (50 to <60 and >/=60 years). Cox proportional adjusted hazard ratios (HRs) were constructed for time to all-cause mortality according to achieved mean SBP. In those 50 to <60 years and using a referent SBP of <130 mm Hg, an achieved SBP of 130 to 140 mm Hg was associated with a similar risk of mortality (HR, 1.03; 95% confidence interval [CI], 0.87-1.23), whereas an achieved SBP of >/=140 mm Hg was associated with an increased risk of mortality (HR, 1.80; 95% CI, 1.53-2.11). Among subjects aged >/=60 years and using a referent SBP of <130 mm Hg, an achieved SBP 130 to 140 mm Hg was associated with a lower mortality risk (HR, 0.92; 95% CI, 0.85-0.98). There was an increased risk of mortality with an achieved SBP >/=150 mm Hg (HR, 1.34; 95% CI, 1.23-1.45), but not with an achieved SBP 140 to 150 mm Hg (HR, 1.02; 95% CI, 0.94-1.11). In hypertensive patients with coronary artery disease, achieving a SBP of 130 to 140 mm Hg seems to be associated with lower all-cause mortality after approximately 11.6 years of follow-up. CLINICAL TRIAL REGISTRATION: URL: http://www.clinicaltrials.gov. Unique identifier: NCT00133692.
CES1P1 variant -816A>C is not associated with hepatic carboxylesterase 1 expression and activity or antihypertensive effect of trandolapril.[Pubmed:26915813]
Eur J Clin Pharmacol. 2016 Jun;72(6):681-7.
PURPOSE: The majority of angiotensin-converting enzyme inhibitors (ACEIs) are synthesized as ester prodrugs that must be converted to their active forms in vivo in order to exert therapeutic effects. Hepatic carboxylesterase 1 (CES1) is the primary enzyme responsible for the bioactivation of ACEI prodrugs in humans. The genetic variant -816A>C (rs3785161) is a common variant located in the promoter region of the CES1P1 gene. Previous studies report conflicting results with regard to the association of this variant and therapeutic outcomes of CES1 substrate drugs. The purpose of this study was to determine the effect of the variant -816A>C on the activation of the ACEI prodrug Trandolapril in human livers and the blood pressure (BP)-lowering effect of Trandolapril in hypertensive patients. METHODS: The -816A>C genotypes and CES1 expression and activity on Trandolapril activation were determined in 100 individual human liver samples. Furthermore, the association of the -816A>C variant and the BP lowering effect of Trandolapril was evaluated in hypertensive patients who participated in the International Verapamil SR Trandolapril Study (INVEST). RESULTS: Our in vitro study demonstrated that hepatic CES1 expression and activity did not differ among different -816A>C genotypes. Moreover, we were unable to identify a clinical association between the BP lowering effects of Trandolapril and -816A>C genotypes. CONCLUSIONS: We conclude that the -816A>C variant is not associated with interindividual variability in CES1 expression and activity or therapeutic response to ACEI prodrugs.
