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75450-34-9

75450-34-9 structure
75450-34-9 structure
  • Name: CGP 37157
  • Chemical Name: 7-chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2-one
  • CAS Number: 75450-34-9
  • Molecular Formula: C15H11Cl2NOS
  • Molecular Weight: 324.225
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Na+/Ca2+ Exchanger
  • Create Date: 2017-01-12 04:05:55
  • Modify Date: 2024-01-10 14:52:51
  • 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.
Name 7-chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2-one
Synonyms 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
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
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.
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℃
Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning
Hazard Statements H302-H400
Precautionary Statements P273
RIDADR UN 3077 9 / PGIII
HS Code 2934999090
74067-45-1 structure

74067-45-1

2365-48-2 structure

2365-48-2

~49%

75450-34-9 structure

75450-34-9

Literature: Pei, Yazhong; Lilly, Michael J.; Owen, David J.; D'Souza, Lawrence J.; Tang, Xiao-Qing; Yu, Jinghua; Nazarbaghi, Ramina; Hunter, Andrew; Anderson, Christen M.; Glasco, Susan; Ede, Nicholas J.; James, Ian W.; Maitra, Uday; Chandrasekaran; Moos, Walter H.; Ghosh, Soumitra S. Journal of Organic Chemistry, 2003 , vol. 68, # 1 p. 92 - 103
488828-86-0 structure

488828-86-0

~%

75450-34-9 structure

75450-34-9

Literature: Pei, Yazhong; Lilly, Michael J.; Owen, David J.; D'Souza, Lawrence J.; Tang, Xiao-Qing; Yu, Jinghua; Nazarbaghi, Ramina; Hunter, Andrew; Anderson, Christen M.; Glasco, Susan; Ede, Nicholas J.; James, Ian W.; Maitra, Uday; Chandrasekaran; Moos, Walter H.; Ghosh, Soumitra S. Journal of Organic Chemistry, 2003 , vol. 68, # 1 p. 92 - 103
74067-45-1 structure

74067-45-1

~%

75450-34-9 structure

75450-34-9

Literature: Pei, Yazhong; Lilly, Michael J.; Owen, David J.; D'Souza, Lawrence J.; Tang, Xiao-Qing; Yu, Jinghua; Nazarbaghi, Ramina; Hunter, Andrew; Anderson, Christen M.; Glasco, Susan; Ede, Nicholas J.; James, Ian W.; Maitra, Uday; Chandrasekaran; Moos, Walter H.; Ghosh, Soumitra S. Journal of Organic Chemistry, 2003 , vol. 68, # 1 p. 92 - 103
488828-36-0 structure

488828-36-0

~%

75450-34-9 structure

75450-34-9

Literature: Pei, Yazhong; Lilly, Michael J.; Owen, David J.; D'Souza, Lawrence J.; Tang, Xiao-Qing; Yu, Jinghua; Nazarbaghi, Ramina; Hunter, Andrew; Anderson, Christen M.; Glasco, Susan; Ede, Nicholas J.; James, Ian W.; Maitra, Uday; Chandrasekaran; Moos, Walter H.; Ghosh, Soumitra S. Journal of Organic Chemistry, 2003 , vol. 68, # 1 p. 92 - 103
Precursor  2

DownStream  0

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

Chemsrc provides CAS#:75450-34-9 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 75450-34-9 | Chemsrc address: https://www.chemsrc.com/en/baike/753850.html

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