Captopril
Based on 23 publication(s) in Google Scholar
Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 62571-86-2
- Formula: C9H15NO3S
- Molecular Weight:217.29
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Captopril
More- Nat Commun. 2023 May 2;14(1):2523. [Abstract]
- Allergy. 2025 Nov 14. [Abstract]
- Phytomedicine. 2025 Sep 15:148:157263. [Abstract]
- Phytomedicine. 2024 May:127:155467. [Abstract]
- Phytomedicine. 2023 Dec:121:155118. [Abstract]
- Apoptosis. 2024 Oct;29(9-10):1499-1514. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Biomed Pharmacother. 2024 Jun 20:177:117012. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Eur J Med Chem. 2022 Mar 5:231:114121. [Abstract]
- Mar Drugs. 2023 Sep 29;21(10):522. [Abstract]
- Eur J Pharmacol. 2025 Aug 6:1005:178045. [Abstract]
- Eur J Pharmacol. 2022 May 15;923:174892. [Abstract]
- Eur J Pharmacol. 2022 Apr 15:921:174871. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- J Cell Mol Med. 2022 Aug;26(16):4548-4555. [Abstract]
- Am J Physiol Heart Circ Physiol. 2018 Mar 1;314(3):H580-H592. [Abstract]
- Sci Rep. 2021 Mar 4;11(1):5241. [Abstract]
- Front Oncol. 2021 Jun 16;11:663671. [Abstract]
- J Orthop Surg Res. 2024 Feb 19;19(1):147. [Abstract]
- Arch Physiol Biochem. 2025 Apr;131(2):285-292. [Abstract]
- Medicine. 2023 Dec 15;102(50):e36177. [Abstract]
- bioRxiv. 2026 Jun 19.
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In Vivo Efficacy Study
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Histological Imaging/Staining
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In Vivo Efficacy Study
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Histological Imaging/Staining
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In Vivo Efficacy Study
Biological Activity
ACE[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
130 μM
Compound: L-A1
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Cytotoxicity against human HeLa cells incubated for 72 hrs by alamar blue cell viability assay
Cytotoxicity against human HeLa cells incubated for 72 hrs by alamar blue cell viability assay
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[PMID: 39013490] |
| KB 3-1 | IC50 |
15.67 mM
Compound: captropril
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Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay
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[PMID: 21657271] |
| KB-V1 | IC50 |
13.07 mM
Compound: captropril
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Cytotoxicity against drug-resistant human KBV1 cells expressing P-gp incubated for 72 hrs by MTT assay
Cytotoxicity against drug-resistant human KBV1 cells expressing P-gp incubated for 72 hrs by MTT assay
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[PMID: 21657271] |
Captopril (SQ 14225) has been shown to have similar morbidity and mortality benefits to those of diuretics and beta-blockers in hypertensive patients. Captopril has been shown to delay the progression of diabetic nephropathy, and enalapril and lisinopril prevent the development of nephropathy in normoalbuminuric patients with diabetes[4].
An equimolar ratio of the cis and trans states of Captopril exists in solution and that the enzyme selects only the trans state of the inhibitor that presents architectural and stereoelectronic complementarity with its substrate binding groove[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 62571-86-2
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Appearance Solid
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Molecular Weight 217.29
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Formula C9H15NO3S
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Color White to yellow
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SMILES
O=C(O)[C@H]1N(C([C@H](C)CS)=O)CCC1
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Synonyms
SQ 14225
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (23)
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Journal Impact Factor
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Most Recent
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Nat Commun
Reduced hepatic bradykinin degradation accounts for cold-induced BAT thermogenesis and WAT browning in male mice. [Abstract]2023 May 2;14(1):2523. PMID: 37130842
Captopril purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 2;14(1):2523. [Abstract]
Serum BK levels from sWAT from WT male mice treated with 40 mg/kg/day Captopril or 70 mg/kg/day Enalapril by gavage once a day for 21 days. The results showed that Captopril significantly increased serum BK levels.
Captopril purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 2;14(1):2523. [Abstract]
Representative immunohistochemistry (IHC) staining of UCP1 and H&E staining of sWAT. Captopril (40 mg/kg; once daily; 21 days; 25°C) induced sWAT brownin.
Captopril purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 2;14(1):2523. [Abstract]
Captopril (40 mg/kg; once daily; 21 days; 25°C) decreased the weight of sWAT in WT male mice.
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Allergy
Long-Term Attenuation of Vascular Hyperpermeability in a Hereditary Angioedema Mouse Model by Adenine Base Editing. [Abstract]2025 Nov 14. PMID: 41236489
Captopril purchased from MedChemExpress. Usage Cited in: Allergy. 2025 Nov 14. [Abstract]
Representative images of feet collected 30 min post-Evans Blue (EB) injection. Mice were assigned to five groups: WT control, Serping1+/− control, WT + Captopril (2.5 mg/kg; i.v.), Serping1+/− + Captopril + PBS, and Serping1+/− + Captopril + AAV-NG-ABE8e. Captopril elicited significant Evans blue leakage.
Captopril purchased from MedChemExpress. Usage Cited in: Allergy. 2025 Nov 14. [Abstract]
Representative intravital confocal images showing real-time FITC-dextran extravasation from intestinal microvasculature. Mice were assigned to: WT control, Serping1+/− control, WT + Captopril (2.5 mg/kg; i.v.), Serping1+/− + Captopril + PBS, and Serping1+/− + Captopril + AAV-NG-ABE8e. By 30 min, Captopril-treated mice demonstrated pronounced FITC-dextran extravasation—both in area and fluorescence intensity—relative to WT and Serping1+/− controls.
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Phytomedicine
Shexiang baoxin pill ameliorates cardiac fibrosis by inhibiting fibroblast to myofibroblast transition through STAT3 phosphorylation suppression. [Abstract]2025 Sep 15:148:157263. PMID: 40975042 -
Phytomedicine
Quercitrin improves cardiac remodeling following myocardial infarction by regulating macrophage polarization and metabolic reprogramming. [Abstract]2024 May:127:155467. PMID: 38447360 -
Phytomedicine
Ethyl ferulate suppresses post-myocardial infarction myocardial fibrosis by inhibiting transforming growth factor receptor 1. [Abstract]2023 Dec:121:155118. PMID: 37801895 -
Apoptosis
Targeting PAX8 sensitizes ovarian cancer cells to ferroptosis by inhibiting glutathione synthesis. [Abstract]2024 Oct;29(9-10):1499-1514. PMID: 38853202 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Biomed Pharmacother
Caffeic acid mitigates myocardial fibrosis and improves heart function in post-myocardial infarction by inhibiting transforming growth factor-β receptor 1 signaling pathways. [Abstract]2024 Jun 20:177:117012. PMID: 38906025 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Eur J Med Chem
Development of targeted nanoparticles loaded with antiviral drugs for SARS-CoV-2 inhibition. [Abstract]2022 Mar 5:231:114121. PMID: 35114539 -
Mar Drugs
Affinity Purification and Molecular Characterization of Angiotensin-Converting Enzyme (ACE)-Inhibitory Peptides from Takifugu flavidus. [Abstract]2023 Sep 29;21(10):522. PMID: 37888457 -
Eur J Pharmacol
Captopril alleviates radiation-induced pulmonary fibrosis by suppressing PAI-1 expression and cytoskeleton-dependent epithelial-to-mesenchymal transition. [Abstract]2025 Aug 6:1005:178045. PMID: 40780595 -
Eur J Pharmacol
Montelukast, cysteinyl leukotriene receptor 1 antagonist, inhibits cardiac fibrosis by activating APJ. [Abstract]2022 May 15;923:174892. PMID: 35358494 -
Eur J Pharmacol
Captopril alleviates glucocorticoid-induced osteonecrosis of the femoral head by mediating the ACE2/ Ang-(1-7)/Mas receptor cascade. [Abstract]2022 Apr 15:921:174871. PMID: 35283112 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
J Cell Mol Med
Pirfenidone alleviates cardiac fibrosis induced by pressure overload via inhibiting TGF-β1/Smad3 signalling pathway. [Abstract]2022 Aug;26(16):4548-4555. PMID: 35861038 -
Am J Physiol Heart Circ Physiol
Overexpression of the neuronal human (pro)renin receptor mediates angiotensin II-independent blood pressure regulation in the central nervous system. [Abstract]2018 Mar 1;314(3):H580-H592. PMID: 29350998 -
Sci Rep
Effect of captopril on post-infarction remodelling visualized by light sheet microscopy and echocardiography. [Abstract]2021 Mar 4;11(1):5241. PMID: 33664407 -
Front Oncol
The Angiotensin-Converting Enzyme Inhibitory State Promotes the Transformation of Non-Small Cell Lung Cancer Blood Supply Pattern Toward Vasculogenic Mimicry Formation. [Abstract]2021 Jun 16;11:663671. PMID: 34221978 -
J Orthop Surg Res
Several first-line anti-hypertensives act on fibrosarcoma progression and PD1ab blockade therapy. [Abstract]2024 Feb 19;19(1):147. PMID: 38373964 -
Arch Physiol Biochem
Huaiqihuang (HQH) protects podocytes from high glucose-induced apoptosis and inflammation response by regulating PI3K/AKT/mTOR pathway. [Abstract]2025 Apr;131(2):285-292. PMID: 39329410 -
Medicine
Mechanism of Huaiqihuang in treatment of diabetic kidney disease based on network pharmacology, molecular docking and in vitro experiment. [Abstract]2023 Dec 15;102(50):e36177. PMID: 38115276 -
Solvent & Solubility
DMSO : ≥ 50 mg/mL (230.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (230.11 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (11.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (11.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 32.5 mg/mL (149.57 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[3]. Li N, et al. Simplified captopril analogues as NDM-1 inhibitors. Bioorg Med Chem Lett. 2014;24(1):386-389. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 4.6021 mL | 23.0107 mL | 46.0214 mL | 115.0536 mL |
| 5 mM | 0.9204 mL | 4.6021 mL | 9.2043 mL | 23.0107 mL | |
| 10 mM | 0.4602 mL | 2.3011 mL | 4.6021 mL | 11.5054 mL | |
| 15 mM | 0.3068 mL | 1.5340 mL | 3.0681 mL | 7.6702 mL | |
| 20 mM | 0.2301 mL | 1.1505 mL | 2.3011 mL | 5.7527 mL | |
| 25 mM | 0.1841 mL | 0.9204 mL | 1.8409 mL | 4.6021 mL | |
| 30 mM | 0.1534 mL | 0.7670 mL | 1.5340 mL | 3.8351 mL | |
| 40 mM | 0.1151 mL | 0.5753 mL | 1.1505 mL | 2.8763 mL | |
| 50 mM | 0.0920 mL | 0.4602 mL | 0.9204 mL | 2.3011 mL | |
| 60 mM | 0.0767 mL | 0.3835 mL | 0.7670 mL | 1.9176 mL | |
| 80 mM | 0.0575 mL | 0.2876 mL | 0.5753 mL | 1.4382 mL | |
| 100 mM | 0.0460 mL | 0.2301 mL | 0.4602 mL | 1.1505 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.