CGP37157
Based on 9 publication(s) in Google Scholar
CGP37157 is a potent, selective inhibitor of Na+/Ca2+ exchanger, inhibiting the Na+-induced Ca2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM.
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- Pureza: 99.87%
- No. CAS: 75450-34-9
- Fòrmula: C15H11Cl2NOS
- Peso molecular:324.22
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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- Referencias
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Publications Citing Use of MedChemExpress (MCE) CGP37157
More- Nature. 2024 Jul;631(8022):826-834. [Abstract]
- Cell Res. 2022 Jul;32(7):638-658. [Abstract]
- Appl Phys Rev. 2026 Jan 21.
- Phytomedicine. 2025 Dec:149:157494. [Abstract]
- Clin Sci. 2025 Oct 22;139(20):1163-1185. [Abstract]
- Cell Rep. 2024 Sep 28;43(10):114794. [Abstract]
- Ecotoxicol Environ Saf. 2024 Jan 1:269:115906. [Abstract]
- Thromb Haemost. 2025 Mar 6. [Abstract]
- J Cell Physiol. 2021 Sep;236(9):6548-6558. [Abstract]
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Cell Imaging/Staining
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Cell Imaging/Staining
Actividad biológica
IC50: 0.8 μM (Na+/Ca2+ exchanger)[1]
CGP37157 (Compound XVI) is a potent, selective inhibitor of Na+/Ca2+ exchanger, inhibiting the Na+-induced Ca2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM[1].
CGP37157 (10 μM) shows inhibitory effect on mitochondrial Na+/Ca2+ exchanger in cortical neurons, modulates intracellular Ca2+ levels via suppresssing voltage-gated calcium channels, and reduces NMDA-induced cytosolic and mitochondrial Ca2+ overloads. CGP37157 (10 μM) also reduces NMDA-induced excitotoxicity, and such an effect is via attenuating mitochondrial damage and calpain activity in neurons[2].
CGP37157 (10 μM) in combination with salinomycin significantly attenuates cell viability and increases apoptosis of FaDu and HLaC79 cells. Moreover, CGP37157 has no inhibitory effect on salinomycin tumor toxicity[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 75450-34-9
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Appearance Solid
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Peso molecular 324.22
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Fòrmula C15H11Cl2NOS
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Color White to off-white
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SMILES
O=C1NC2=CC=C(Cl)C=C2C(C3=CC=CC=C3Cl)SC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Nature
2024 Jul;631(8022):826-834. PMID: 38987597
CGP37157 purchased from MedChemExpress. Usage Cited in: Nature. 2024 Jul;631(8022):826-834. [Abstract]
[Ca2+]i changes of primary cultured cortical neurons imaged from Asic1a+/+ mice (n = 20–26 cells from 3 cultures per group). 200 μM glutamate, 10 μM LY341495 (mGluRs blockers), 10 μM CGP37157 (inhibitor of Na+/Ca2+ exchanger in mitochondria), 10 μM RO2959 (selective Ca2+ release-activated Ca2+ channel inhibitor) and 100 ng/ml PcTX-1 were applied.
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Cell Res
SLC1A1-mediated cellular and mitochondrial influx of R-2-hydroxyglutarate in vascular endothelial cells promotes tumor angiogenesis in IDH1-mutant solid tumors. [Abstract]2022 Jul;32(7):638-658. PMID: 35459936
CGP37157 purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Jul;32(7):638-658. [Abstract]
OCR measurement. HUVECs were treated with R-2-HG (10 mM) plus CGP-37157 (10 μM) for 1 h.
CGP37157 purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Jul;32(7):638-658. [Abstract]
Aortic ring sprouting assay. Matrigel-ring mixture was treated with R-2-HG (10 mM) plus CGP-37157 (10 μM) for 7 days.
CGP37157 purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Jul;32(7):638-658. [Abstract]
The impact of the mitochondrial respiration, Na+/Ca2+ exchange and R-2-HG uptake on F-actin formation. HUVECs were treated with R-2-HG (10 mM) alone or in combination with CGP-37157 (10 μM) for 1 h.
CGP37157 purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Jul;32(7):638-658. [Abstract]
R-2-HG-induced mitochondrial migration in HUVECs. Cells were treated with R-2-HG (10 mM) and CGP-37157 (10 μM) at the indicated time-points. Mitochondria were visualized by MitoTracker Red. Shown were snapshots of fluorescence images of time-lapse videos of mitochondrial redistribution.
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Phytomedicine
Z-Ligustilide's antidepressant effects in adolescent depression involve the PTEN-induced putative kinase 1 (PINK1) - protein kinase A (PKA)- Na+/Ca2+ exchanger (NCLX) pathway, facilitating mitochondrial endosymbiosis and promoting mitophagy in microglia. [Abstract]2025 Dec:149:157494. PMID: 41218379 -
Clin Sci
Glutamine alleviates immunosuppression in polymicrobial sepsis by augmenting bacterial phagocytosis through sustaining the GFAT-DRP1 dependent mitochondrial calcium dynamics. [Abstract]2025 Oct 22;139(20):1163-1185. PMID: 41082631 -
Cell Rep
Mitotic ER-mitochondria contact enhances mitochondrial Ca2+ influx to promote cell division. [Abstract]2024 Sep 28;43(10):114794. PMID: 39342616 -
Ecotoxicol Environ Saf
MicroRNA-129-1-3p protects chicken granulosa cells from cadmium-induced apoptosis by down-regulating the MCU-mediated Ca2+ signaling pathway. [Abstract]2024 Jan 1:269:115906. PMID: 38176135 -
Thromb Haemost
Inhibition of IP3 (Inositol 1,4,5-Trisphosphate) Receptors Retards SARS-CoV-2-Induced Endothelial von Willebrand Factor Secretion and Thrombosis. [Abstract]2025 Mar 6. PMID: 40049586 -
J Cell Physiol
Effects of various calcium transporters on mitochondrial Ca2+ changes and oocyte maturation. [Abstract]2021 Sep;236(9):6548-6558. PMID: 33704771
Solvente y solubilidad
DMSO : ≥ 125 mg/mL (385.53 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 (7.71 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.
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.
Protocolo
Cell toxicity assays are performed. Neurons are exposed to NMDA in HBSS (free of Ca2+ and Mg2+) containing 2.6 mM CaCl2, 10 mM glucose and 10 μM glycine for 10 or 30 min at 37°C, depending on the experiment. CGP37157 is present before and during the excitotoxic insult and cell viability is assessed 24 h later using Citotox 96 colorimetric assay. All experiments are performed in quadruplicate and the values provided are the normalized mean ± S.E.M. of at least three independent experiments[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (285 KB)
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SDS (536 KB)
- English - EN (536 KB)
- Français - FR (536 KB)
- Deutsch - DE (536 KB)
- Norwegian - NO (536 KB)
- Español - ES (536 KB)
- Swedish - SV (536 KB)
- Italian - IT (536 KB)
- Korean - KR (536 KB)
- Portuguese - PT (536 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Chiesi M, et al. Structural dependency of the inhibitory action of benzodiazepines and related compounds on the mitochondrial Na+-Ca2+ exchanger. Biochem Pharmacol. 1988 Nov 15;37(22):4399-403. [Content Brief]
[2]. Ruiz A, et al. CGP37157, an inhibitor of the mitochondrial Na+/Ca2+ exchanger, protects neurons from excitotoxicity by blocking voltage-gated Ca2+ channels. Cell Death Dis. 2014 Apr 10;5:e1156. [Content Brief]
[3]. Scherzed A, et al. Effects of salinomycin and CGP37157 on head and neck squamous cell carcinoma cell lines in vitro. Mol Med Rep. 2015 Sep;12(3):4455-61. [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 | 3.0843 mL | 15.4214 mL | 30.8428 mL | 77.1070 mL |
| 5 mM | 0.6169 mL | 3.0843 mL | 6.1686 mL | 15.4214 mL | |
| 10 mM | 0.3084 mL | 1.5421 mL | 3.0843 mL | 7.7107 mL | |
| 15 mM | 0.2056 mL | 1.0281 mL | 2.0562 mL | 5.1405 mL | |
| 20 mM | 0.1542 mL | 0.7711 mL | 1.5421 mL | 3.8553 mL | |
| 25 mM | 0.1234 mL | 0.6169 mL | 1.2337 mL | 3.0843 mL | |
| 30 mM | 0.1028 mL | 0.5140 mL | 1.0281 mL | 2.5702 mL | |
| 40 mM | 0.0771 mL | 0.3855 mL | 0.7711 mL | 1.9277 mL | |
| 50 mM | 0.0617 mL | 0.3084 mL | 0.6169 mL | 1.5421 mL | |
| 60 mM | 0.0514 mL | 0.2570 mL | 0.5140 mL | 1.2851 mL | |
| 80 mM | 0.0386 mL | 0.1928 mL | 0.3855 mL | 0.9638 mL | |
| 100 mM | 0.0308 mL | 0.1542 mL | 0.3084 mL | 0.7711 mL |
CGP37157 Related Classifications
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