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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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Purity: ≥98%
Perindopril Erbumine (also called S9490-3; Pirindopril; ACEON; Perindopril tert-butylamine; Perstarium), the tert-butylamine salt of perindopril, is a long acting and brain penetrant ACE (angiotensin-converting enzyme) inhibitor with anti-hypertensive effects. It inhibits ACE with an IC50 of 1.05 nM and has been approved for use in the treatment of hypertension and heart failure. Perindopril Erbumine can suppress the increase in hippocampal ACE activity and improves cognition in PS2APP-transgenic mice. Perindopril Erbumine displays a higher binding affinity for the bradykinin binding sites than the angiotensin I binding sites of ACE. Perindopril Erbumine inhibits the angiotensin- and Aβ42-to-Aβ40-converting activity of mutated ACE containing two active domains (F-ACE) with IC50 of 0.03-0.1 μM, and 0.01-0.03 μM, respectively.
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| ln Vivo |
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| Animal Protocol |
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Limited information indicates that only low levels of perindopril and its active metabolite are found in breastmilk, which is consistent with other drugs in this class. Amounts ingested by the infant are small and would not be expected to cause any adverse effects in breastfed infants. ◉ Effects in Breastfed Infants Ten infants were breastfed (extent not stated) by mothers were taking perindopril 5 to 20 mg daily. All infants grew and developed normally according to their parents. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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| References |
Eur J Pharmacol.2007 Dec 22;577(1-3):1-6;J Biol Chem.2009 Nov 13;284(46):31914-20.
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| Additional Infomation |
Perindopril erbumine is an addition compound. It has a role as an antihypertensive agent and an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor. It contains a perindopril(1-).
Perindopril Erbumine is the tert-butylamine salt of perindopril, the ethyl ester of a non-sulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Upon hydrolysis, perindopril erbumine is converted to its active form perindoprilat, inhibiting ACE and 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. An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure. See also: Perindopril (has active moiety); Perindoprilat (has active moiety). |
| Molecular Formula |
C19H32N2O5.C4H11N
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| Molecular Weight |
441.6
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| Exact Mass |
441.32
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| CAS # |
107133-36-8
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| Related CAS # |
Perindopril;82834-16-0
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| PubChem CID |
441313
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| Appearance |
White to off-white solid powder
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| Density |
1.15 g/cm3
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| Boiling Point |
537.4ºC at 760mmHg
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| Melting Point |
126-128ºC
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| Flash Point |
278.8ºC
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| LogP |
3.713
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
31
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| Complexity |
549
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CCC[C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@H]2CCCC[C@H]2C[C@H]1C(=O)O.CC(C)(C)N
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| InChi Key |
IYNMDWMQHSMDDE-MHXJNQAMSA-N
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| InChi Code |
InChI=1S/C19H32N2O5.C4H11N/c1-4-8-14(19(25)26-5-2)20-12(3)17(22)21-15-10-7-6-9-13(15)11-16(21)18(23)24;1-4(2,3)5/h12-16,20H,4-11H2,1-3H3,(H,23,24);5H2,1-3H3/t12-,13-,14-,15-,16-;/m0./s1
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| Chemical Name |
(2S,3aS,7aS)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxopentan-2-yl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid;2-methylpropan-2-amine
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| Synonyms |
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (226.45 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
Solubility in Formulation 2: Saline: 30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2645 mL | 11.3225 mL | 22.6449 mL | |
| 5 mM | 0.4529 mL | 2.2645 mL | 4.5290 mL | |
| 10 mM | 0.2264 mL | 1.1322 mL | 2.2645 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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