| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Captopril (SQ 14225; SA333) is a potent angiotensin-converting enzyme (ACE) inhibitor with IC50 of 6 nM. It is the prototypical drug in the ACE class with antihypertensive efficacy commonly used in the control of blood pressure. Captopril has been shown to be an inhibitor of ACE1, but not ACE2. Captopril is also a reversible and competitive inhibitor of leukotriene A4 hydrolase. Administration of captopril inhibits the pressor response to intravenously administered angiotensin I but not that induced by angiotensin II both in normal human beings and in conscious normotensive rabbits. Captopril is proven to be a useful alternative to combination antihypertensive therapy.
| ln Vitro |
It has been demonstrated that in individuals with hypertension, captopril (SQ 14225) has a similar morbidity and effectiveness to diuretics and beta-blockers. It has been demonstrated that captopril slows the advancement of diabetic nephropathy, but enalapril and lisinopril stop the disease's progression in patients with normoalbuminuric diabetes [4]. The solution contains equimolar ratios of captopril in both its cis and trans states, with the enzyme exclusively choosing the trans form of the compound. The enzyme and its substrate binding base exhibit structural and stereoelectronic complementarity [5].
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| References |
[1]. Afrin S, et al. Eritadenine from Edible Mushrooms Inhibits Activity of Angiotensin Converting Enzyme in Vitro. J Agric Food Chem. 2016;64(11):2263-2268.
[2]. Esmaeili S, et al. Captopril/enalapril inhibit promiscuous esterase activity of carbonic anhydrase at micromolar concentrations: An in vitro study. Chem Biol Interact. 2017;265:24-35. [3]. Li N, et al. Simplified captopril analogues as NDM-1 inhibitors. Bioorg Med Chem Lett. 2014;24(1):386-389. [4]. Tzakos, A.G., et al., The molecular basis for the selection of captopril cis and trans conformations by angiotensin I converting enzyme. Bioorg Med Chem Lett, 2006. 16(19): p. 5084-7. [5]. Song, J.C. and C.M. White, Clinical pharmacokinetics and selective pharmacodynamics of new angiotensin converting enzyme inhibitors: an update. Clin Pharmacokinet, 2002. 41(3): p. 207-24. |
| Molecular Formula |
C9H15NO3S
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| Molecular Weight |
217.29
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| CAS # |
62571-86-2
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| Related CAS # |
Captopril hydrochloride;198342-23-3;Captopril-d3;1356383-38-4
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| SMILES |
S([H])C([H])([H])[C@@]([H])(C([H])([H])[H])C(N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(=O)O[H])=O
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| InChi Key |
FAKRSMQSSFJEIM-BQBZGAKWSA-N
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| InChi Code |
InChI=1S/C9H15NO3S/c1-6(5-14)8(11)10-4-2-3-7(10)9(12)13/h6-7,14H,2-5H2,1H3,(H,12,13)/t6-,7-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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: ≥ 2.5 mg/mL (11.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 32.5 mg/mL (149.57 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6021 mL | 23.0107 mL | 46.0214 mL | |
| 5 mM | 0.9204 mL | 4.6021 mL | 9.2043 mL | |
| 10 mM | 0.4602 mL | 2.3011 mL | 4.6021 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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