Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
1g |
Purity: ≥98%
Fosinopril (SQ28555, Monopril), the ester prodrug of fosinoprilat, is a potent angiotensin-converting enzyme (ACE) inhibitor that is used for the treatment of hypertension and some types of chronic heart failure. It has to be converted to its active metabolite fosinoprilat. Fosinopril is a phosphinic acid-containing ACE inhibitor that is effective in the treatment of hypertension. Fosinopril binds 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 (0-100 μM; 30 min) [1]. There is no inhibitory effect of fosinopril (250 nM) on the soluble esterase activity of LPLA2 [1]. The ACE activity is non-competitively inhibited by fosinopril (0.372, 0.744, 1.116 μM), with a Ki value of 1.675 μM [2].
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ln Vivo |
Rats given fosinopril (4.67 mg/kg; oral; 4 weeks) have reduced levels of creatine kinase (CK) and lactate dehydrogenase (LDH), as well as protection against structural alterations and cardiac dysfunction [3]. In the AMI rat model, fosinopril (4.67 mg/kg; oral; 4 weeks) can suppress the production of cleaved-caspase 3 and cardiomyocyte apoptosis [3].
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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: po (oral gavage); 4 weeks Experimental Results: Inhibition of cardiac dysfunction and structural changes and inhibition of 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 |
C30H46NO7P
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Molecular Weight |
563.66254
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CAS # |
98048-97-6
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Related CAS # |
Fosinopril sodium;88889-14-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(O)[C@@H]1N(C(CP(CCCCC2=CC=CC=C2)(OC(OC(CC)=O)C(C)C)=O)=O)C[C@@H](C3CCCCC3)C1
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InChi Key |
BIDNLKIUORFRQP-KKDZQFHASA-N
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InChi Code |
InChI=1S/C30H46NO7P/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)/t25-,26+,30?,39?/m0/s1
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Chemical Name |
(2R,4R)-4-cyclohexyl-1-(2-((2-methyl-1-(propionyloxy)propoxy)(4-phenylbutyl)phosphoryl)acetyl)pyrrolidine-2-carboxylic
acid
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Synonyms |
SQ-28555SQ28555SQ 28555
FosinoprilMonopril
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.7741 mL | 8.8706 mL | 17.7412 mL | |
5 mM | 0.3548 mL | 1.7741 mL | 3.5482 mL | |
10 mM | 0.1774 mL | 0.8871 mL | 1.7741 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.