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Product Details

CGP-37157 | MPTP inhibitor

CGP-37157 (75450-34-9) inhibits the mitochondrial Na+-Ca2+ exchanger (NCX) in isolated heart mitochondria, IC50=0.36 mM.1 Does not inhibit the plasmalemmal NCX.2  Also inhibits voltage-gated Ca2+ channels in intact cells and therefore its use in cellular studies must employ adequate controls.3  Prevents sudden death in a Guinea pig model of heart failure.4 Displays pronounced cytoprotective effects in chromaffin cells5 and in neuronal injury models.6 Blood-brain barrier permeant.

 

References

1) Cox et al. (1993), Selectivity of inhibition of Na(+)-Ca2+ exchange of heart mitochondria by benzothiazepine CGP-37157; J. Cardiovasc. Pharmacol., 21 595
2) Namekata et al. (2015), Pharmacological discrimination of plasmalemmal and mitochondrial sodium-calcium exchanger in cardiomyocyte-derived H9c2 cells; Biol. Pharm. Bull, 38 147
3) Baron & Thayer (1997), CGP37157 modulates mitochondrial Ca2+ homeostasis in cultured rat dorsal root ganglion neurons; Eur. J. Pharmacol., 340 295
4) Liu et al. (2014), Inhibiting mitochondrial Na+/Ca2+ exchange prevents sudden death in a guinea pig model of heart failure; Circ. Res., 115 44
5) Nicolau et al. (2009), Mitochondrial Na+/Ca2+-exchanger blocker CGP37157 protects against chromaffin cell death elicited by veratridine; J. Pharmacol. Exp. Ther., 330 844
6) Ruiz et al. (2014), CGP37157, an inhibitor of the mitochondrial Na+/Ca2+ exchanger, protects neurons from excitotoxicity by blocking voltage gated Ca2+ channels; Cell Death Dis., 5 e1156

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Catalog#  10-4250

$80.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
75450-34-9
Catalog Number:
10-4250
Activity:
MPTP inhibitor
Chemical Name:
7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one
Molecular Weight:
324.22
Molecular Formula:
C15H11Cl2NOS
Solubility:
Soluble in DMSO (up to 25 mg/ml).
Physical Properties:
White solid
Purity:
99% by TLC
Storage Temperature:
RT
Stability:
Stable for 2 years as supplied
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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