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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Fosinopril Sodium (also known as SQ28555), the ester prodrug offosinoprilat, is a potent angiotensin-converting enzyme (ACE) inhibitor that is used for the treatment of hypertension and some types of chronic heart failure. Fosinopril Sodium is a phosphinic acid-containing ACEinhibitor that is effective in the treatment of hypertension. Fosinoprilbinds to the active site of ACE via targeting the zinc ions with its phosphinic acid moiety.
| ln Vitro |
Co-sedimentation of liposomes and recombinant LPLA2 is partially inhibited by fosinopril (0, 1, 10, 33, 100 μM; 30 min) [1]. The soluble esterase activity of LPLA2 is not inhibited by fosinopril (250 nM) [1]. With a Ki value of 1.675 μM, fosinopril (0.372, 0.744, 1.116 μM) inhibits ACE activity in a non-competitive manner [2].
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| ln Vivo |
By decreasing the levels of lactate dehydrogenase (LDH) and creatine kinase (CK), fosinopril (oral; 4.67 mg/kg; 4 weeks) counteracts cardiac dysfunction and structural alterations [3]. In rat models of acute myocardial infarction, fosinopril (oral; 4.67 mg/kg; 4 weeks) reduces the expression of cleaved-caspase 3 and cardiomyocyte apoptosis.
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| Animal Protocol |
Animal/Disease Models: Acute myocardial infarction (AMI) rat model after heart failure (SPF grade SD (SD (Sprague-Dawley)) rat, 265±15g) [3]
Doses: 4.67mg/kg Route of Administration: oral; 4-week Experimental Results: Combats cardiac dysfunction and structural changes and inhibits apoptosis. |
| References |
[1]. Ondetti, M.A., Structural relationships of angiotensin converting-enzyme inhibitors to pharmacologic activity. Circulation, 1988. 77(6 Pt 2): p. I74-8.
[2]. Piepho, R.W., Overview of the angiotensin-converting-enzyme inhibitors. Am J Health Syst Pharm, 2000. 57 Suppl 1: p. S3-7. [3]. Sharma, S., et al., The hemodynamic effects of long-term ACE inhibition with fosinopril in patients with heart failure. Fosinopril Hemodynamics Study Group. Am J Ther, 1999. 6(4): p. 181-9. |
| Molecular Formula |
C30H45NO7P.NA
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|---|---|
| Molecular Weight |
585.64
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| CAS # |
88889-14-9
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| Related CAS # |
Fosinopril;98048-97-6
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| SMILES |
P(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])(C([H])([H])C(N1[C@]([H])(C(=O)[O-])C([H])([H])[C@]([H])(C1([H])[H])C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])=O)(=O)OC([H])(C([H])(C([H])([H])[H])C([H])([H])[H])OC(C([H])([H])C([H])([H])[H])=O.[Na+]
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| InChi Key |
TVTJZMHAIQQZTL-HREVRLCXSA-M
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| InChi Code |
InChI=1S/C30H46NO7P.Na/c1-4-28(33)37-30(22(2)3)38-39(36,18-12-11-15-23-13-7-5-8-14-23)21-27(32)31-20-25(19-26(31)29(34)35)24-16-9-6-10-17-24;/h5,7-8,13-14,22,24-26,30H,4,6,9-12,15-21H2,1-3H3,(H,34,35);/q;+1/p-1/t25-,26+,30?,39?;/m1./s1
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| Chemical Name |
sodium;(2S,4S)-4-cyclohexyl-1-[2-[(2-methyl-1-propanoyloxypropoxy)-(4-phenylbutyl)phosphoryl]acetyl]pyrrolidine-2-carboxylate
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| Synonyms |
SQ-28,555;SQ 28,555; SQ 28555; SQ-28,555; SQ-28555; SQ28,555; SQ28555; Monopril; Staril; Dynacil; Fosinil; Tenso Stop; Tensocardil; Sodium, Fosinopril; Staril;
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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:<1 mg/mL
Water:117 mg/mL (199.8 mM)
Ethanol:4 mg/mL (6.8 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 9.09 mg/mL (15.52 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7075 mL | 8.5377 mL | 17.0753 mL | |
| 5 mM | 0.3415 mL | 1.7075 mL | 3.4151 mL | |
| 10 mM | 0.1708 mL | 0.8538 mL | 1.7075 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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