CGP37157

SKU: orb1308461

Description

CGP37157 is a potent Na+/Ca2+ exchanger (NCX) inhibitor with an IC50 of 0.8 μM for blocking Na+-induced mitochondrial Ca2+ release in guinea pig hearts. This small molecule is a valuable research tool for studying calcium homeostasis and NCX function in cardiac physiology and pathophysiology, both in vitro and in vivo.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 75450-34-9
• MW: 324.22
• Purity: 99.92%
• Formula: C₁₅H₁₁Cl₂NOS
• SMILES: Clc1ccc2NC(=O)CSC(c3ccccc3Cl)c2c1
• Target: Na+/Ca2+ Exchanger
• Solubility: DMSO:150 mg/mL (462.65 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.17 mM)

Bioactivity

• Target IC50:
  Na+, Ca2+ exchanger:0.8 μM
• In Vitro:
  Administration of 10 μM CGP37157 shows an inhibitory effect on mitochondrial Na+/Ca2+ exchanger in cortical neurons, modulating intracellular Ca2+ levels via suppressing voltage-gated calcium channels. Administration of 10 μM CGP37157 in combination with salinomycin significantly attenuates cell viability and increases apoptosis of FaDu and HLaC79 cells. CGP37157 has no inhibitory effect on salinomycin tumor toxicity. Administration of 10 μM CGP37157 reduces NMDA-induced cytosolic and mitochondrial Ca2+ overloads and it also reduces NMDA-induced excitotoxicity, and such an effect is via attenuating mitochondrial damage and calpain activity in neurons.

Storage & Handling

• Storage: Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CGP 37157, CGP37157, CGP-37157, 7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one, Ca2+ Exchanger, Ca2+Exchanger, Inhibitor, inhibit, Na+ Exchanger, Na+/Ca2+ exchanger, Na+Exchanger, Na+/Ca2+ Exchanger

Compound Identifiers

PubChem CID

2688