Cariporide
Based on 12 publication(s) in Google Scholar
Cariporide (HOE-642) is a selective Na+/H+ exchange inhibitor.
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 159138-80-4
- Formula: C12H17N3O3S
- Molecular Weight:283.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Cariporide
More- Acta Pharm Sin B. 2023 Apr;13(4):1671-1685. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Hum Reprod. 2024 Apr 3;39(4):674-688. [Abstract]
- JCI Insight. 2023 Oct 9;8(19):e170928. [Abstract]
- Drug Des Devel Ther. 2026 May 12:20:585989. [Abstract]
- Am J Pathol. 2024 Aug 31:S0002-9440(24)00328-6. [Abstract]
- iScience. 2026 Feb 19;29(3).
- FASEB J. 2019 Jun;33(6):7202-7212. [Abstract]
- Am J Physiol Heart Circ Physiol. 2024 Feb 1;326(2):H418-H425. [Abstract]
- Biomed Pharmacother. 2025 Oct 22:192:118670. [Abstract]
- Res Sq. 2024 Jun 11.
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Cell Imaging/Staining
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Others
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Cell Imaging/Staining
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IF
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Others
Biological Activity
Cariporide significantly suppresses markers of cell death, such as TUNEL positivity and caspase-3 cleavage, at 8 or 16 hours. Cariporide remarkably suppresses cytosolic Na+ and Ca2+ accumulation. Cariporide prevents mitochondrial membrane potential loss induced by H2+O2+[1].
Cariporide (HOE-642) ameliorates myocardial ischemia/reperfusion injury, by the well-established reduction of cytosolic Ca2+ in cardiac myocytes through inhibition of Na+/H+ exchange[2].
Cariporide (HOE-642), has inhibitory effects on the degranulation of human platelets, the formation of platelet–leukocyte-aggregates, and the activation of the GPIIb/IIIa receptor (PAC-1)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 159138-80-4
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Appearance Solid
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Molecular Weight 283.35
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Formula C12H17N3O3S
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Color White to off-white
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SMILES
O=C(NC(N)=N)C1=CC=C(C(C)C)C(S(=O)(C)=O)=C1
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Synonyms
HOE-642 Free Base
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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 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Acta Pharm Sin B
Structural repurposing of SGLT2 inhibitor empagliflozin for strengthening anti-heart failure activity with lower glycosuria. [Abstract]2023 Apr;13(4):1671-1685. PMID: 37139418 -
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 -
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 -
Hum Reprod
Flagellar pH homeostasis mediated by Na+/H+ exchangers regulates human sperm functions through coupling with CatSper and KSper activation. [Abstract]2024 Apr 3;39(4):674-688. PMID: 38366201 -
JCI Insight
Acid-base homeostasis orchestrated by NHE1 defines pancreatic stellate cell phenotype in pancreatic cancer. [Abstract]2023 Oct 9;8(19):e170928. PMID: 37643024
Cariporide purchased from MedChemExpress. Usage Cited in: JCI Insight. 2023 Oct 9;8(19):e170928. [Abstract]
Immunocytochemistry of PDAC-like PSCs in the absence (left) or presence (right) of cariporide (CARI: 10 μM).
Cariporide purchased from MedChemExpress. Usage Cited in: JCI Insight. 2023 Oct 9;8(19):e170928. [Abstract]
Immunocytochemistry of CAFs derived from KPfC mice after a 1-month treatment with vehicle or gemcitabine + Cariporide (3 mg/kg i.p.).
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Drug Des Devel Ther
GBVAM as a Novel NHE1 Inhibitor Alleviates Doxorubicin-Induced Cardiotoxicity via PI3K/Akt/mTOR Pathway. [Abstract]2026 May 12:20:585989. PMID: 42148365 -
Am J Pathol
Lipopolysaccharide Triggers Luminal Acidification to Promote Defense Against Bacterial Infection in Vaginal Epithelium. [Abstract]2024 Aug 31:S0002-9440(24)00328-6. PMID: 39222908
Cariporide purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2024 Aug 31:S0002-9440(24)00328-6. [Abstract]
Statistical analysis showing the effect of Cariporide (10 μmol/L) on the enhanced pHi recovery induced by LPS (10 μg/mL) stimulation for 6 hours in VK2/E6E7 cells.
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FASEB J
AMP-activated protein kinase regulates glycocalyx impairment and macrophage recruitment in response to low shear stress. [Abstract]2019 Jun;33(6):7202-7212. PMID: 30860864 -
Am J Physiol Heart Circ Physiol
Empagliflozin treatment rescues abnormally reduced Na currents in ventricular cardiomyocytes from dystrophin-deficient mdx mice. [Abstract]2024 Feb 1;326(2):H418-H425. PMID: 38099845
Cariporide purchased from MedChemExpress. Usage Cited in: Am J Physiol Heart Circ Physiol. 2024 Feb 1;326(2):H418-H425. [Abstract]
original current traces of a control mdx (mdx DMSO), a cariporide-treated mdx (mdx CARI, 24-h incubation at 10 µM concentration), and a cariporide-plus EMPA-treated (mdx CARI + EMPA) cardiomyocyte.
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Biomed Pharmacother
Sodium glucose co-transporter 2 inhibitor empagliflozin prevents endothelial dysfunction induced by oscillatory shear stress. [Abstract]2025 Oct 22:192:118670. PMID: 41130096
Cariporide purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Oct 22:192:118670. [Abstract]
To test the involvement of NHE1 and NCX in the ROS inhibition effect of EMPA, HCAECs were pre-incubated with either Vehicle, Cariporide (10 µM) or ORM-10962 (100 nM), in combination with EMPA or not, for 2 h before exposure to OSS. After 6 h, ROS was measured using live cell image and quantified with MFI.
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Solvent & Solubility
DMSO : ≥ 100 mg/mL (352.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (8.82 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 (8.82 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Neonatal rat cardiomyocytes are randomly separated into groups: (1) control group, (2) incubation with 100 μM hydrogen peroxide, or (3) pretreatment with 10 μM cariporide for 20 minutes followed by 100 μM hydrogen peroxide. Caspase-3 activity is measured by detection of the cleavage of a colorimetric caspase-3 substrate, N-acetyl-Asp-Glu-Val-Asp-p-nitroaniline, using an assay kit[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats: Cariporide and/or bumetanide are administered intravenously (15 or 30 mg/kg in 2 to 4 doses, respectively, of 7.5 mg/kg) starting at 20 minutes before initiation of pMCAO. For neurologic outcome experiments, some rats are given cariporide and/or bumetanide by a single intraperitoneal injection[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Teshima Y, et al. Cariporide (HOE642), a selective Na+-H+ exchange inhibitor, inhibits the mitochondrial death pathway. Circulation. 2003 Nov 4;108(18):2275-81. [Content Brief]
[2]. Chang HB, et al. Na(+)/H(+) exchanger in the regulation of platelet activation and paradoxical effects of cariporide. Exp Neurol. 2015 Oct;272:11-6. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5292 mL | 17.6460 mL | 35.2920 mL | 88.2301 mL |
| 5 mM | 0.7058 mL | 3.5292 mL | 7.0584 mL | 17.6460 mL | |
| 10 mM | 0.3529 mL | 1.7646 mL | 3.5292 mL | 8.8230 mL | |
| 15 mM | 0.2353 mL | 1.1764 mL | 2.3528 mL | 5.8820 mL | |
| 20 mM | 0.1765 mL | 0.8823 mL | 1.7646 mL | 4.4115 mL | |
| 25 mM | 0.1412 mL | 0.7058 mL | 1.4117 mL | 3.5292 mL | |
| 30 mM | 0.1176 mL | 0.5882 mL | 1.1764 mL | 2.9410 mL | |
| 40 mM | 0.0882 mL | 0.4412 mL | 0.8823 mL | 2.2058 mL | |
| 50 mM | 0.0706 mL | 0.3529 mL | 0.7058 mL | 1.7646 mL | |
| 60 mM | 0.0588 mL | 0.2941 mL | 0.5882 mL | 1.4705 mL | |
| 80 mM | 0.0441 mL | 0.2206 mL | 0.4412 mL | 1.1029 mL | |
| 100 mM | 0.0353 mL | 0.1765 mL | 0.3529 mL | 0.8823 mL |