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5mg |
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ln Vitro |
Enalapril decreases GlySar absorption in a competitive manner, according to kinetic study (Ki = 6 mM). With IC50 values of 55 and 81 μM, respectively, fosinopril and zofenopril have the highest inhibitory potency, while other ACE inhibitors interact with renal peptide transporters with low affinity [1].
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ln Vivo |
When administered intraperitoneally, zolofenopril, a sulfonate molecule, can have a notable protective impact on the tonic phase at doses greater than 70 mg/kg (i.e., 70 mg/kg, P=0.044, F=2.17, df=18; P<0.05 at higher concentrations). Epilepsy responses triggered by sound. Pretreatment with zofenopril (15 mg/kg i.p.) resulted in a considerable reduction in the clonic ED50 of various AEDs (benzofen, felbamate, and diazepam), as well as a consistent shift leftward in the dose-response curve. Compared to concurrent treatment groups, all of the drugs (except from barbiturates and phenytoin) had enhanced anticonvulsant activity [2].
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References |
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Additional Infomation |
Zofenopril is a proline derivative that is 4-(phenylsulfanyl)-L-proline in which the amine proton is replaced by a (2S)-3-(benzoylsulfanyl)-2-methylpropanoyl group. A prodrug for zofenoprilat. It has a role as an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor, an apoptosis inhibitor, a cardioprotective agent, an anticonvulsant, a prodrug and a vasodilator agent. It is a thioester, a N-acyl-L-amino acid, an aryl sulfide and a L-proline derivative. It is a conjugate acid of a zofenopril(1-).
Zofenopril is employed as both a cardioprotective and anti-hypertensive agent. It is an angiotensin-converting enzyme (ACE) inhibitor. Zofenopril is a sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, zofenopril is hydrolyzed in vivo into its active form zofenoprilat. Zofenoprilat 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. Zofenoprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow. |
Molecular Formula |
C22H23NO4S2
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Molecular Weight |
429.5523
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Exact Mass |
429.106
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CAS # |
81872-10-8
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Related CAS # |
Zofenopril-d5;Zofenopril calcium;81938-43-4
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PubChem CID |
92400
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Appearance |
White to off-white solid powder
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Density |
1.3±0.1 g/cm3
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Boiling Point |
646.3±55.0 °C at 760 mmHg
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Melting Point |
129-131.5ºC(lit.)
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Flash Point |
344.7±31.5 °C
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Vapour Pressure |
0.0±2.0 mmHg at 25°C
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Index of Refraction |
1.659
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LogP |
3.78
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Hydrogen Bond Donor Count |
1
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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 |
587
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Defined Atom Stereocenter Count |
3
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SMILES |
C[C@H](CSC(=O)C1=CC=CC=C1)C(=O)N2C[C@H](C[C@H]2C(=O)O)SC3=CC=CC=C3
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InChi Key |
IAIDUHCBNLFXEF-MNEFBYGVSA-N
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InChi Code |
InChI=1S/C22H23NO4S2/c1-15(14-28-22(27)16-8-4-2-5-9-16)20(24)23-13-18(12-19(23)21(25)26)29-17-10-6-3-7-11-17/h2-11,15,18-19H,12-14H2,1H3,(H,25,26)/t15-,18+,19+/m1/s1
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Chemical Name |
(2S,4S)-1-[(2S)-3-benzoylsulfanyl-2-methylpropanoyl]-4-phenylsulfanylpyrrolidine-2-carboxylic acid
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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 : ~5 mg/mL (~11.64 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 | 2.3280 mL | 11.6401 mL | 23.2802 mL | |
5 mM | 0.4656 mL | 2.3280 mL | 4.6560 mL | |
10 mM | 0.2328 mL | 1.1640 mL | 2.3280 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.