[CAS NO. 75450-34-9] CGP37157
PRODUCTS SPECIFICATIONS [75450-34-9]
DESCRIPTION [75450-34-9]
Overview
| MDL | MFCD09055422 |
|---|---|
| Molecular Weight | 324.22 |
| Molecular Formula | C15H11Cl2NOS |
| SMILES | O=C1NC2=CC=C(Cl)C=C2C(C3=CC=CC=C3Cl)SC1 |
2 Publications Citing Use of MCE
Summary
CGP37157 is a potent, selective inhibitor of Na + /Ca 2+ exchanger , inhibiting the Na + -induced Ca 2+ -release from guinea-pig heart mitochondria, with an IC 50 of 0.8 μM.
IC50 & Target
IC50: 0.8 μM (Na + /Ca 2+ exchanger) [1]
In Vitro
CGP37157 (Compound XVI) is a potent, selective inhibitor of Na + /Ca 2+ exchanger, inhibiting the Na + -induced Ca 2+ -release from guinea-pig heart mitochondria, with an IC 50 of 0.8 μM [1] . CGP37157 (10 μM) shows inhibitory effect on mitochondrial Na + /Ca 2+ exchanger in cortical neurons, modulates intracellular Ca 2+ levels via suppresssing voltage-gated calcium channels, and reduces NMDA-induced cytosolic and mitochondrial Ca 2+ 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 125 mg/mL ( 385.54 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 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 |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution
References
- [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.
- [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.
- [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.