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Chemical Structure| 75450-34-9 Chemical Structure| 75450-34-9

Structure of CGP37157
CAS No.: 75450-34-9

Chemical Structure| 75450-34-9

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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.

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Product Details of CGP37157

CAS No. :75450-34-9
Formula : C15H11Cl2NOS
M.W : 324.22
SMILES Code : O=C1NC2=CC=C(Cl)C=C2C(C3=CC=CC=C3Cl)SC1
MDL No. :MFCD09055422

Safety of CGP37157

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H319-H332-H372-H400
Precautionary Statements:P260-P264-P270-P273-P280-P301+P312+P330-P304+P312-P305+P351+P338-P314-P337+P313-P391-P501
Class:9
UN#:3077
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Rat islet cells 0.1 μM CGP37157 restored mitochondrial calcium signaling, ATP generation, and glucose-stimulated insulin secretion in Pdx1-deficient islets Cell Metab. 2009 Aug;10(2):110-8.
hippocampal slices 10 μM 4 h To evaluate the neuroprotective effect of CGP37157 in the glutamate excitotoxicity model. Results showed that CGP37157 increased cell survival in Calhm1+/+ slices but had no significant effect in Calhm1−/− slices. Cells. 2020 Mar 9;9(3):664.
hippocampal slices 10 μM and 30 μM OGD for 15 min, reoxygenation for 2 h To evaluate the neuroprotective effect of CGP37157 in the OGD/Reox model. Results showed that CGP37157 reduced cell death in Calhm1+/+ slices but had no significant effect in Calhm1−/− slices. Cells. 2020 Mar 9;9(3):664.
rat cortical neurons 10μM 1 h To analyze how intracellular Ca2+ levels are modulated by CGP37157 during NMDA insults, it was found that CGP37157 strongly prevented depolarization-induced [Ca2+]i increase by blocking voltage-gated Ca2+ channels (VGCCs), while it did not induce depletion of ER Ca2+ stores. Moreover, mitochondrial Ca2+ overload was reduced as a consequence of diminished Ca2+ entry through VGCCs, leading to attenuation of excitotoxic mitochondrial damage. Cell Death Dis. 2014 Apr 10;5(4):e1156.
mouse embryonic fibroblasts (MEFs) 80 µM 5 min inhibits oligomycin-stimulated glycolytic increase J Cell Biol. 2022 Nov 7;221(11):e202201160.
mouse embryonic fibroblasts (MEFs) 80 µM 3 min inhibits CCCP-induced glycolytic increase J Cell Biol. 2022 Nov 7;221(11):e202201160.
mouse uterine longitudinal smooth muscle cells 10 μM 30 min To investigate the effect of CGP37157 on uterine contractile force, results showed CGP37157 significantly decreased the force of contractions Br J Pharmacol. 2010 Nov;161(6):1375-90.
liver mitochondria 30 µM 30 min To study the inhibitory effect of CGP37157 on Na+-induced Ca2+ efflux Cell Calcium. 2021 Jun;96:102382.
heart mitochondria 30 µM 30 min To study the inhibitory effect of CGP37157 on Na+-induced Ca2+ efflux Cell Calcium. 2021 Jun;96:102382.
brain mitochondria 30 µM 30 min To study the inhibitory effect of CGP37157 on Na+-induced Ca2+ efflux Cell Calcium. 2021 Jun;96:102382.
smooth muscle cells of rat cerebral arteries 10 µM CGP37157, as a mitochondrial Na+–Ca2+ exchange blocker, activated transient KCa currents J Physiol. 2004 May 1;556(Pt 3):755-71.
HEK293 cells 10, 30, 50 μM To test the effects of CGP-37157 on ANO1 and CaV3.2 currents. Results showed that CGP-37157 significantly inhibited ANO1 and CaV3.2 currents. Cell Calcium. 2018 Jun;72:1-17.
brain nonsynaptic mitochondria 10 μM To investigate the effect of CGP37157 on residual Ca2+ uptake in MCU-KO brain mitochondria, results showed no inhibition by CGP37157. J Biol Chem. 2018 Oct 5;293(40):15652-15663.
HeLa cells 10 μM 2 min Inhibited NCLX-mediated Ca2+ extrusion, almost completely prevented Ca2+ efflux J Biol Chem. 2014 Jul 18;289(29):20377-85.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.08mL

0.62mL

0.31mL

15.42mL

3.08mL

1.54mL

30.84mL

6.17mL

3.08mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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