CGP 37157

Modify Date: 2024-01-10 14:52:51

CGP 37157 structure	Common Name	CGP 37157
	CAS Number	75450-34-9	Molecular Weight	324.225
	Density	1.4±0.1 g/cm3	Boiling Point	479.8±45.0 °C at 760 mmHg
	Molecular Formula	C₁₅H₁₁Cl₂NOS	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	244.0±28.7 °C
	Symbol	GHS07, GHS09	Signal Word	Warning

Use of CGP 37157

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
Synonym	More Synonyms

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.

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
Signal Word	Warning
Hazard Statements	H302-H400
Precautionary Statements	P273
RIDADR	UN 3077 9 / PGIII
HS Code	2934999090

2-amino-5-chlor...

CAS#:74067-45-1

Methyl thioglycolate

CAS#:2365-48-2

~49%

CGP 37157

CAS#: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

N/A

CAS#:488828-86-0

CGP 37157

CAS#:75450-34-9

2-amino-5-chlor...

CAS#:74067-45-1

CGP 37157

CAS#:75450-34-9

[(2-amino-5-chl...

CAS#:488828-36-0

CGP 37157

CAS#:75450-34-9

Precursor 2
CAS#:74067-45-1 2-amino-5-chlor... CAS#:2365-48-2 Methyl thioglycolate
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%

Pulsed infrared radiation excites cultured neonatal spiral and vestibular ganglion neurons by modulating mitochondrial calcium cycling.

J. Neurophysiol. 112(6) , 1246-55, (2014)

Cochlear implants are currently the most effective solution for profound sensorineural hearing loss, and vestibular prostheses are under development to treat bilateral vestibulopathies. Electrical cur...

UCP2 modulates single-channel properties of a MCU-dependent Ca(2+) inward current in mitochondria.

Pflugers Arch. 467 , 2509-18, (2015)

The mitochondrial Ca(2+) uniporter is a highly Ca(2+)-selective protein complex that consists of the pore-forming mitochondrial Ca(2+) uniporter protein (MCU), the scaffolding essential MCU regulator ...

Mitochondrial Ca(2+) uniporter (MCU)-dependent and MCU-independent Ca(2+) channels coexist in the inner mitochondrial membrane.

Pflugers Arch. 466(7) , 1411-20, (2014)

A protein referred to as CCDC109A and then renamed to mitochondrial calcium uniporter (MCU) has recently been shown to accomplish mitochondrial Ca(2+) uptake in different cell types. In this study, we...

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

DC Chemicals Limited
China
Product Name: CGP 37157
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/500mg
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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Price: $88/10mM*1mLinDMSO

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CGP 37157

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