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| ln Vitro |
In HNSCC cells, perindoprilat (1 μM) therapy suppresses angiotensin II synthesis for 10 days [2]. Treatment with perindoprilat (40 μM, 3 days) reduced the levels of fibronectin in mesangial cells [3].
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| ln Vivo |
In mice with acute myocardial infarction, perindopril treatment (oral gavage; 1.5 mg/kg; once daily; 7 days) improves cardiac function and decreases the number of apoptotic cardiomyocytes [4]. In mice with acute myocardial infarction, perindopril (oral gavage; 1.5 mg/kg; once daily; 7 d) treatment can decrease myocardial Bax and Bcl-2 expression levels in the infarct area [4]. Mice with acute myocardial infarction can be treated with perindopril (oral gavage; 1.5 mg/kg; once daily; 7 d) to decrease the expression of myocardial TLR4/NF-κB in the infarct area [4].
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| Cell Assay |
Cell viability assay [2]
Cell Types: HNSCC Cell Tested Concentrations: 1 μM Incubation Duration: 10 days Experimental Results: Inhibited angiotensin II production in HNSCC cells (P=0.028). Cell viability assay [3] Cell Types: Human mesangial cells Tested Concentrations: 40 μM Incubation Duration: 3 days Experimental Results: Result in MPCM-stimulated fibronectin levels diminished by 19.4±0.6% (P<0.001) and 21.7±1.0% (P< 0.001) for secreted and cell-associated fibronectin levels, respectively. |
| Animal Protocol |
Animal/Disease Models: C57BL/6J mouse coronary artery ligation [4]
Doses: 1.5 mg/kg Route of Administration: po (oral gavage); 1.5 mg/kg; one time/day; 7 days Experimental Results: Compared with the acute myocardial infarction group, myocardial infarction The number of apoptotic cells was Dramatically diminished (p<0.05). Animal/Disease Models: C57BL/6J mouse coronary artery ligation [4] Doses: 1.5 mg/kg Route of Administration: po (oral gavage); 1.5 mg/kg; one time/day; 7 days Experimental Results: Bax gene in the infarct area of mice with acute myocardial infarction and diminished protein expression levels. Animal/Disease Models: C57BL/6J mouse coronary artery ligation [4] Doses: 1.5 mg/kg Route of Administration: po (oral gavage); 1.5 mg/kg; one time/day; 7 days Experimental Results: Compared with the acute myocardial infarction group, infarction The number of NF-κB p50 protein staining in the nucleus of the area diminished (p<0.05). |
| References | |
| Additional Infomation |
Perindoprilat is a dipeptide obtained by formal condensation of one of the carboxy groups of N-[(1S)-1-carboxyethyl]-L-norvaline with the amino group of (2S,3aS,7aS)-octahydroindole-2-carboxylic acid. The major active metabolite of perindopril. It has a role as an antihypertensive agent, an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor and a drug metabolite. It is an organic heterobicyclic compound, a dipeptide, a dicarboxylic acid and a L-alanine derivative.
The active metabolite of the prodrug [Perindopril]. Perindoprilat is an Angiotensin Converting Enzyme Inhibitor. The mechanism of action of perindoprilat is as an Angiotensin-converting Enzyme Inhibitor. Perindoprilat is a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Perindoprilat inhibits ACE and, thus, the conversion of angiotensin I to angiotensin II; consequently, angiotensin II-mediated vasoconstriction and angiotensin II-stimulated aldosterone secretion from the adrenal cortex are inhibited and diuresis and natriuresis ensue. See also: Perindopril Erbumine (active moiety of). |
| Molecular Formula |
C17H28N2O5
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|---|---|
| Molecular Weight |
340.42
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| Exact Mass |
340.199
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| CAS # |
95153-31-4
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| PubChem CID |
72022
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
568.1±45.0 °C at 760 mmHg
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| Melting Point |
153-155ºC
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| Flash Point |
297.4±28.7 °C
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| Vapour Pressure |
0.0±3.4 mmHg at 25°C
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| Index of Refraction |
1.535
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| LogP |
2.37
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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 |
7
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| Heavy Atom Count |
24
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| Complexity |
495
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CCC[C@@H](C(=O)O)N[C@@H](C)C(=O)N1[C@H]2CCCC[C@H]2C[C@H]1C(=O)O
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| InChi Key |
ODAIHABQVKJNIY-PEDHHIEDSA-N
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| InChi Code |
InChI=1S/C17H28N2O5/c1-3-6-12(16(21)22)18-10(2)15(20)19-13-8-5-4-7-11(13)9-14(19)17(23)24/h10-14,18H,3-9H2,1-2H3,(H,21,22)(H,23,24)/t10-,11-,12-,13-,14-/m0/s1
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| Chemical Name |
(2S,3aS,7aS)-1-[(2S)-2-[[(1S)-1-carboxybutyl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid
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| Synonyms |
Perindoprilate; Perindoprilat
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
H2O : ~250 mg/mL (~734.41 mM)
DMSO : ~125 mg/mL (~367.20 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 | 2.9375 mL | 14.6877 mL | 29.3755 mL | |
| 5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL | |
| 10 mM | 0.2938 mL | 1.4688 mL | 2.9375 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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