1. Membrane Transporter/Ion Channel
  2. Na+/Ca2+ Exchanger
  3. CGP37157

CGP37157 

Cat. No.: HY-15754 Purity: 99.79%
Handling Instructions

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.

For research use only. We do not sell to patients.

CGP37157 Chemical Structure

CGP37157 Chemical Structure

CAS No. : 75450-34-9

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
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10 mg USD 120 In-stock
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25 mg USD 260 In-stock
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50 mg USD 460 In-stock
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100 mg USD 810 In-stock
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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.

IC50 & 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].

Molecular Weight

324.22

Formula

C₁₅H₁₁Cl₂NOS

CAS No.

75450-34-9

SMILES

O=C1NC2=CC=C(Cl)C=C2C(C3=CC=CC=C3Cl)SC1

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
In Vitro: 

DMSO : ≥ 125 mg/mL (385.54 mM)

*"≥" means soluble, but saturation unknown.

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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CGP37157
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HY-15754
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