CGP-37157 | MPTP inhibitor

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
NMR (conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solution in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size :PriceQuantity 
10 mg$70.00
50 mg$270.00

CGP-37157 (75450-34-9) inhibits the mitochondrial Na+-Ca2+ exchanger (NCX) in isolated heart mitochondria, IC50=0.36 µM.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/Citations:

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

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
NMR (conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solution in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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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