CGP 37157

Names

[ Name ]:
CGP 37157

[Synonym ]:
7-CHLORO-5-(2-CHLOROPHENYL)-1,5-DIHYDRO-4,1-BENZOTHIAZEPIN-2(3H)-ONE
PF9 tetrasodium salt
4,1-Benzothiazepin-2(3H)-one, 7-chloro-5-(2-chlorophenyl)-1,5-dihydro-
CGP37157

Biological Activity

[Description]:

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.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Na+/Ca2+ Exchanger

Research Areas >> Cancer

Research Areas >> Neurological Disease

[Target]

IC50: 0.8 μM (Na+/Ca2+ exchanger)[1]

[In Vitro]

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].

[Cell Assay]

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].

[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.

[Related Small Molecules]

KB-R7943 mesylate | SEA-0400 | SN6 | SM-6586 | Caldaret

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
479.8±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₅H₁₁Cl₂NOS

[ Molecular Weight ]:
324.225

[ Flash Point ]:
244.0±28.7 °C

[ Exact Mass ]:
322.993835

[ PSA ]:
54.40000

[ LogP ]:
5.02

[ Vapour Pressure ]:
0.0±1.2 mmHg at 25°C

[ Index of Refraction ]:
1.640

[ Storage condition ]:
2-8℃

Safety Information

[ Symbol ]:

GHS07, GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H400

[ Precautionary Statements ]:
P273

[ RIDADR ]:
UN 3077 9 / PGIII

[ HS Code ]:
2934999090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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