| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Zofenopril calcium targets angiotensin-converting enzyme (ACE), which is responsible for converting angiotensin I to the potent vasoconstrictor angiotensin II. By inhibiting ACE, zofenopril reduces angiotensin II production, leading to vasodilation and decreased blood pressure. The compound also targets PEPT2, the predominant peptide transporter in kidney and choroid plexus. The sulfhydryl group in zofenoprilat contributes to its cardioprotective effects beyond ACE inhibition. Zofenopril also functions as an antioxidant.
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| ln Vitro |
Zofenopril calcium exhibits ACE inhibitory activity in vitro, with its active metabolite zofenoprilat binding to the ACE active site. The compound's antioxidant properties have been demonstrated in biochemical assays. Studies indicate that zofenopril calcium increases the calcium cycling of sarcoplasmic reticulum and enhances active calcium uptake into the sarcoplasmic reticulum. These effects contribute to its cardioprotective activity. The compound's inhibition of PEPT2 has been characterized in transport assays.
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| ln Vivo |
Zofenopril calcium has been studied in healthy volunteers for its pharmacokinetics and pharmacodynamics. A single oral dose of 60 mg in healthy volunteers demonstrated the compound's ACE inhibitory activity and antihypertensive effects. The compound's cardioprotective effect has been demonstrated in clinical studies. Zofenopril is used for the treatment of acute myocardial infarction. Its efficacy as an antihypertensive agent has been well established.
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| Enzyme Assay |
In vitro enzyme assays for zofenopril calcium involve measuring the inhibition of angiotensin-converting enzyme (ACE) activity using purified ACE and appropriate substrates. The compound is first converted to its active metabolite zofenoprilat, and the inhibition of ACE-mediated angiotensin I conversion is measured. PEPT2 inhibition assays are performed using transport assays with labeled substrates. Antioxidant activity is assessed using standard cell-free assays such as DPPH radical scavenging. These assays provide mechanistic insights into the compound's pharmacological activities.
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| Cell Assay |
In vitro cell-based assays for zofenopril calcium involve treating cells with the compound to assess its effects on ACE activity, calcium cycling, and oxidative stress. Endothelial cells or smooth muscle cells are treated with zofenopril, and ACE activity is measured. Calcium cycling in sarcoplasmic reticulum is assessed using fluorescent calcium indicators. Antioxidant effects are evaluated by measuring reactive oxygen species levels. Cell viability and function are assessed using standard assays. These cellular studies characterize the compound's protective effects.
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| Animal Protocol |
In vivo animal experiments for zofenopril calcium have been conducted in models of hypertension and myocardial infarction. Hypertensive animals are treated with zofenopril orally, and blood pressure is monitored. Cardioprotective effects are assessed in models of myocardial ischemia/reperfusion injury. Efficacy endpoints include blood pressure reduction, infarct size reduction, and biomarker analysis. Pharmacokinetic studies have been performed in healthy volunteers.
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| ADME/Pharmacokinetics |
Zofenopril calcium is a prodrug that is hydrolyzed in vivo into its active form, zofenoprilat. It is a long-acting, lipophilic ACE inhibitor. Following oral administration (e.g., 60 mg single dose), the compound is absorbed and converted to zofenoprilat. The pharmacokinetic profile has been characterized in healthy volunteers. The compound's lipophilicity contributes to its tissue distribution and duration of action. It is primarily eliminated through renal and biliary routes.
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| Toxicity/Toxicokinetics |
The toxicity profile of zofenopril calcium is characteristic of ACE inhibitors. Common adverse effects include cough, hypotension, and hyperkalemia. The compound's sulfhydryl group may contribute to a lower incidence of cough compared to other ACE inhibitors. Preclinical toxicology studies have established the safety profile for clinical use. The compound is contraindicated in patients with a history of angioedema related to ACE inhibitor therapy.
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| References |
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| Additional Infomation |
Zofenopril calcium is an organic calcium salt, a hemicalcium salt of Zofenopril, and a prodrug of Zofenopril. It possesses anticonvulsant, anti-apoptotic, cardioprotective, EC 3.4.15.1 (peptidyl dipeptidase A) inhibitor, prodrug, and vasodilatory effects. It contains the Zofenopril (1-) domain. Zofenopril calcium is the calcium salt of Zofenopril, a thiol-angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, Zofenopril is hydrolyzed in vivo to its active form, Zofenopril. Zofenopril competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the strong vasoconstrictive effect of angiotensin II, leading to vasodilation. Zofenopril can also reduce adrenal cortex aldosterone secretion for angiotensin II, thereby increasing sodium excretion and consequently increasing water excretion.
Zofenopril calcium is a second-generation ACE inhibitor with antihypertensive and cardioprotective effects. It is a prodrug that is hydrolyzed to the active sulfhydryl-containing metabolite zofenoprilat. Zofenopril is a long-acting, lipophilic ACE inhibitor. In addition to ACE inhibition, it exhibits antioxidant properties and increases calcium cycling in the sarcoplasmic reticulum. The compound is used for the treatment of acute myocardial infarction and hypertension. |
| Molecular Formula |
C22H22CA0.5NO4S2
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|---|---|
| Molecular Weight |
448.58
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| Exact Mass |
896.16
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| CAS # |
81938-43-4
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| Related CAS # |
Zofenopril;81872-10-8
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| PubChem CID |
3033690
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| Appearance |
White to off-white solid powder
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| Density |
1.34 g/cm3
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| Boiling Point |
646.3ºC at 760 mmHg
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| Melting Point |
>250ºC
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| Flash Point |
344.7ºC
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| LogP |
7.806
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
59
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| Complexity |
582
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| Defined Atom Stereocenter Count |
6
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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.C[C@H](CSC(=O)C1=CC=CC=C1)C(=O)N2C[C@H](C[C@H]2C(=O)[O-])SC3=CC=CC=C3.[Ca+2]
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| InChi Key |
NSYUKKYYVFVMST-LETVYOFWSA-L
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| InChi Code |
InChI=1S/2C22H23NO4S2.Ca/c2*1-15(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*2-11,15,18-19H,12-14H2,1H3,(H,25,26);/q;;+2/p-2/t2*15-,18+,19+;/m11./s1
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| Chemical Name |
calcium;(2S,4S)-1-[(2S)-3-benzoylsulfanyl-2-methylpropanoyl]-4-phenylsulfanylpyrrolidine-2-carboxylate
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| Synonyms |
SQ26991 Zoprace SQ-26991 SQ 26991
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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. |
| 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 : ~2 mg/mL (~4.46 mM)
H2O : < 0.1 mg/mL |
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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 | 2.2293 mL | 11.1463 mL | 22.2926 mL | |
| 5 mM | 0.4459 mL | 2.2293 mL | 4.4585 mL | |
| 10 mM | 0.2229 mL | 1.1146 mL | 2.2293 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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