| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
CGP 37157 targets the mitochondrial Na+/Ca2+ exchanger (mNCX), a transporter that mediates the exchange of Na+ and Ca2+ across the inner mitochondrial membrane. By inhibiting this exchanger, CGP 37157 prevents the efflux of Ca2+ from mitochondria, leading to increased mitochondrial Ca2+ levels.
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| ln Vitro |
Compound XVI, also known as CGP37157, is a strong and tailored activator of the Na+/Ca2+ exchange that, with an IC50 of 0.8 μM, prevents Na+-induced Ca2+ release from guinea pig heart mitochondria [1]. By blocking voltage-gated calcium channels, CGP37157 (10 μM) inhibits the mitochondrial Na+/Ca2+ exchanger in cortical neurons, lowers cytosolic and mitochondrial Ca2+ overload brought on by NMDA, and controls intracellular Ca2+ levels. 10 μM of CGP37157 Mango lessens the excitotoxicity caused by NMDA When CGP37157 (10 μM) and salinomycin were coupled, FaDu and HLaC79 cells' chamber sizes rose and their vitality was considerably decreased. The toxicity of tumor cells is not inhibited by salinomycin [3].
In vitro, CGP 37157 inhibits the activity of the mitochondrial Na+/Ca2+ exchanger with an IC50 of 360 nM. It also inhibits sarcoplasmic reticulum calcium-stimulated ATPase and possibly other calcium channels. The compound is cell-permeable and does not compete with ATP. |
| ln Vivo |
In vivo, CGP 37157 has been used to study the role of mitochondrial calcium handling in various physiological and pathological processes. By inhibiting the mitochondrial Na+/Ca2+ exchanger, it can modulate mitochondrial calcium levels and affect cellular metabolism, apoptosis, and neuroprotection. Specific in vivo data are available from published studies.
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| Enzyme Assay |
In vitro enzyme assays for mitochondrial Na+/Ca2+ exchange typically use isolated mitochondria or mitoplasts. Mitochondria are loaded with a Ca2+-sensitive fluorescent dye (e.g., Calcium Green or Rhod-2), and the rate of Na+-dependent Ca2+ efflux is measured in the presence of varying concentrations of CGP 37157. IC50 values for inhibition of Ca2+ efflux are calculated from dose-response curves.
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| Cell Assay |
In vitro cellular assays for mitochondrial Na+/Ca2+ exchange inhibitors typically use neuronal or cardiac cell lines. Cells are loaded with Ca2+-sensitive dyes, and mitochondrial Ca2+ levels are measured using confocal microscopy or fluorescence plate readers. Cells are treated with CGP 37157 at various concentrations, and the effect on mitochondrial Ca2+ dynamics is assessed.
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| Animal Protocol |
In vivo animal studies for mitochondrial Na+/Ca2+ exchange inhibitors typically use rodent models of ischemia, neurodegeneration, or cardiac disease. Animals are administered CGP 37157 via various routes, and mitochondrial function, tissue damage, and functional outcomes are assessed. Specific protocols are available from published studies on the compound's effects.
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| ADME/Pharmacokinetics |
CGP 37157 is a cell-permeable small molecule that can cross biological membranes. It has a molecular weight of 324.22 and is soluble in DMSO. The compound is metabolized in the liver, and its metabolites are excreted via the kidneys. Detailed PK parameters such as half-life, Cmax, and AUC are available from preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of CGP 37157 would typically include acute and repeated-dose toxicity in rodents, as well as genotoxicity and safety pharmacology assessments. As a modulator of mitochondrial calcium handling, potential effects on cellular metabolism and apoptosis should be monitored. The compound is generally well-tolerated at therapeutic doses.
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| References |
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| Additional Infomation |
7-Chloro-5-(2-Chlorophenyl)-1,5-dihydro-4,1-benzothiazoline-2-one is a benzothiazoline.
CGP 37157 is a potent and selective inhibitor of the mitochondrial Na+/Ca2+ exchanger with an IC50 of 360 nM. It is a benzothiazepine compound that is cell-permeable. The compound is used as a research tool to study mitochondrial calcium handling and is available for research use only. |
| Molecular Formula |
C15H11CL2NOS
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|---|---|
| Molecular Weight |
324.22
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| Exact Mass |
322.993
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| CAS # |
75450-34-9
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| PubChem CID |
2688
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
479.8±45.0 °C at 760 mmHg
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| Flash Point |
244.0±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.640
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| LogP |
5.02
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
368
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KQEPIRKXSUIUTH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11Cl2NOS/c16-9-5-6-13-11(7-9)15(20-8-14(19)18-13)10-3-1-2-4-12(10)17/h1-7,15H,8H2,(H,18,19)
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| Chemical Name |
7-chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2-one
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| Synonyms |
Cgp37157; Cgp-37157; Cgp 37157
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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 |
| 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 : ≥ 125 mg/mL (~385.54 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.71 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 (7.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0843 mL | 15.4216 mL | 30.8433 mL | |
| 5 mM | 0.6169 mL | 3.0843 mL | 6.1687 mL | |
| 10 mM | 0.3084 mL | 1.5422 mL | 3.0843 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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