| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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Purity: ≥98%
Trandolaprilat is a non-sulfhydryl and potent angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Trandolaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation.
| 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 |
Trandolaprilat is a heterobicyclic compound that is trandolapril in which the ethyl ester group has been hydrolysed to the corresponding acid group. It is the active metabolite of the prodrug trandolapril. It has a role as an antihypertensive agent, an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor, a drug metabolite and a human xenobiotic metabolite. It is an organic heterobicyclic compound, a dipeptide, a secondary amino compound, a tertiary carboxamide and a dicarboxylic acid.
The active metabolite of the prodrug [Trandolapril]. Trandolaprilat is an Angiotensin Converting Enzyme Inhibitor. The mechanism of action of trandolaprilat is as an Angiotensin-converting Enzyme Inhibitor. Trandolaprilat is a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Trandolaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Trandolaprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow. See also: Trandolapril (active moiety of); Trandolapril hydrochloride (is active moiety of). |
| 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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