| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Angiotensin-converting enzyme (ACE). Trandolaprilat competitively binds to and inhibits ACE, blocking the conversion of angiotensin I to angiotensin II. It has sub-nanomolar affinity with an IC₅₀ of 0.57 nM for human somatic ACE.
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| ln Vitro |
In vitro, Trandolaprilat shows potent ACE inhibitory activity with an IC₅₀ of 0.57 nM for human somatic ACE. It competitively binds to and inhibits ACE, blocking the conversion of angiotensin I to angiotensin II. The compound partially inhibits angiotensin-I-mediated c-fos induction. It shows high lipophilicity (log kw7.4 = 1.487), facilitating vascular, renal, and cardiac tissue penetration.
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| ln Vivo |
In vivo, Trandolaprilat exerts its pharmacological effect by inhibiting the conversion of angiotensin I to angiotensin II, leading to vasodilation and reduced blood pressure. As the active metabolite of trandolapril, it is responsible for the drug's long-acting antihypertensive effects. The compound's high lipophilicity facilitates tissue ACE occupancy in vascular, renal, and cardiac tissues.
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| Enzyme Assay |
Non-cell enzyme assays are performed using recombinant human somatic ACE. The enzyme is incubated with a fluorogenic or chromogenic substrate (e.g., Abz-Gly-p-nitro-Phe-Pro-OH) and varying concentrations of Trandolaprilat (0.001-100 nM). The reaction is carried out in assay buffer at 37°C for 30-60 minutes. Fluorescence or absorbance is measured, and the IC₅₀ is calculated from dose-response curves. The compound's high affinity (IC₅₀ = 0.57 nM) makes it a critical standard for enzyme kinetics and binding displacement assays.
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| Cell Assay |
Cellular assays for ACE inhibition are performed using ACE-expressing cell lines (e.g., endothelial cells). Cells are treated with Trandolaprilat at concentrations ranging from 0.01-1000 nM. Angiotensin I conversion to angiotensin II is measured by ELISA or LC-MS/MS. The inhibition of angiotensin-II-mediated cellular responses (e.g., calcium mobilization, gene expression) is assessed. IC₅₀ values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies are conducted in rodent models of hypertension (e.g., spontaneously hypertensive rats). Trandolaprilat or its prodrug trandolapril is administered orally or intravenously at doses ranging from 0.1-10 mg/kg. Blood pressure is measured by tail-cuff or telemetry. ACE activity in plasma and tissues is assessed by enzyme activity assays. Tissue distribution studies are performed to evaluate organ-specific ACE occupancy.
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| ADME/Pharmacokinetics |
Trandolaprilat is the active diacid metabolite of the prodrug trandolapril. It has a molecular weight of 402.5 g/mol and a molecular formula of C22H30N2O5. The compound shows high lipophilicity (log kw7.4 = 1.487). It is typically stored at -20°C and shipped under ambient conditions. Trandolaprilat is used as an analytical-grade reference standard for LC-MS/MS method validation and pharmacokinetic quantification of trandolapril.
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| Toxicity/Toxicokinetics |
Trandolaprilat is generally well tolerated at therapeutic doses. As an ACE inhibitor, it may cause hypotension, hyperkalemia, cough, and angioedema in susceptible individuals. No significant genotoxicity or carcinogenicity has been reported. The compound is contraindicated during pregnancy due to the risk of fetal toxicity. Standard safety pharmacology studies have been conducted for the parent drug trandolapril.
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| References |
: Pharmacokinetics, Pharmacodynamics, and Tolerability of Single and Multiple Doses of Trandolapril, an Effective Angiotensin-Converting Enzyme Inhibitor, in Healthy Chinese Subjects. Eur J Drug Metab Pharmacokinet. 2016 Aug;41(4):373-84. doi: 10.1007/s13318-015-0277-2. PubMed PMID: 25864194.
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| Additional Infomation |
Tridopril is a heterobicyclic compound, a product of the hydrolysis of the ethyl ester group of tripopril to the corresponding acid group. It is the active metabolite of the prodrug tripopril. It possesses multiple functions, including antihypertensive activity, inhibition of EC 3.4.15.1 (peptidyl dipeptidase A) activity, and function as a drug metabolite and human xenobiotic metabolite. It is an organic heterobicyclic compound belonging to the dipeptide, secondary amino compound, tertiary amide, and dicarboxylic acid classes. Tridopril is the active metabolite of the prodrug tripopril. Tridopril is an angiotensin-converting enzyme inhibitor. The mechanism of action of tripopril is as an angiotensin-converting enzyme inhibitor. Tridopril is a non-thiol angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Tridopril competitively binds to and inhibits the activity of ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive effect of angiotensin II, leading to vasodilation. Tridopril can also reduce adrenal cortex's aldosterone secretion in response to angiotensin II, thereby increasing sodium excretion and consequently increasing water excretion. See also: Tridopril (active ingredient); Tridopril hydrochloride (active ingredient).
Trandolaprilat is the active metabolite of the ACE inhibitor prodrug trandolapril. It belongs to the class of nonsulfhydryl ACE inhibitors. The compound's high lipophilicity facilitates tissue penetration and long-acting antihypertensive effects. Trandolapril is approved for the treatment of hypertension and heart failure. Trandolaprilat is used as a research tool and reference standard for studying ACE inhibition. |
| Molecular Formula |
C22H30N2O5
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|---|---|
| Molecular Weight |
402.48
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| Exact Mass |
402.215
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| CAS # |
87679-71-8
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| Related CAS # |
Trandolaprilate hydrate;951393-55-8;Trandolaprilate-d5;1356841-27-4;Trandolaprilate-d6
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| PubChem CID |
5464097
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.247 g/cm3
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| Boiling Point |
640.5ºC at 760 mmHg
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| Melting Point |
132-134ºC
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| Flash Point |
341.2ºC
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| LogP |
2.623
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
29
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| Complexity |
604
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C(N1[C@H](C(=O)O)C[C@H]2CCCC[C@H]12)(=O)[C@H](C)N[C@H](C(=O)O)CCC1C=CC=CC=1
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| InChi Key |
AHYHTSYNOHNUSH-HXFGRODQSA-N
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| InChi Code |
InChI=1S/C22H30N2O5/c1-14(23-17(21(26)27)12-11-15-7-3-2-4-8-15)20(25)24-18-10-6-5-9-16(18)13-19(24)22(28)29/h2-4,7-8,14,16-19,23H,5-6,9-13H2,1H3,(H,26,27)(H,28,29)/t14-,16+,17-,18-,19-/m0/s1
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| Chemical Name |
(2S,3aR,7aS)-1-(((S)-1-carboxy-3-phenylpropyl)-L-alanyl)octahydro-1H-indole-2-carboxylic acid
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| Synonyms |
Trandolaprilate RU 44403 RU44403 RU-44403 Trandolapril diacid, Trandolapril Related Compound E,
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ~125 mg/mL (~310.57 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4846 mL | 12.4230 mL | 24.8460 mL | |
| 5 mM | 0.4969 mL | 2.4846 mL | 4.9692 mL | |
| 10 mM | 0.2485 mL | 1.2423 mL | 2.4846 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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