CGP 37157 - CAS 75450-34-9
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
CGP 37157 is a a selective sodium-calcium exchanger inhibitor with IC50 value of 0.36 μM in isolated mitochondria. It does not affect channels, exchangers, or ATPases on the cardiac sarcolemma or ATPases on sarcoplasmic reticulum. CGP 37157 can be used to study the role of mitochondrial-derived calcium in cytoplasmic calcium homeostasis.
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CGP 37157;7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one
DMSO: ≥20 mg/mL
-20℃ Freezer
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
1.Functional reconstitution of the mitochondrial Ca2+/H+ antiporter Letm1.
Tsai MF1, Jiang D, Zhao L, Clapham D, Miller C. J Gen Physiol. 2014 Jan;143(1):67-73. doi: 10.1085/jgp.201311096. Epub 2013 Dec 16.
The leucine zipper, EF hand-containing transmembrane protein 1 (Letm1) gene encodes a mitochondrial inner membrane protein, whose depletion severely perturbs mitochondrial Ca(2+) and K(+) homeostasis. Here we expressed, purified, and reconstituted human Letm1 protein in liposomes. Using Ca(2+) fluorophore and (45)Ca(2+)-based assays, we demonstrate directly that Letm1 is a Ca(2+) transporter, with apparent affinities of cations in the sequence of Ca(2+) ≈ Mn(2+) > Gd(3+) ≈ La(3+) > Sr(2+) >> Ba(2+), Mg(2+), K(+), Na(+). Kinetic analysis yields a Letm1 turnover rate of 2 Ca(2+)/s and a Km of ∼25 µM. Further experiments show that Letm1 mediates electroneutral 1 Ca(2+)/2 H(+) antiport. Letm1 is insensitive to ruthenium red, an inhibitor of the mitochondrial calcium uniporter, and CGP-37157, an inhibitor of the mitochondrial Na(+)/Ca(2+) exchanger. Functional properties of Letm1 described here are remarkably similar to those of the H(+)-dependent Ca(2+) transport mechanism identified in intact mitochondria.
2.Mitochondrial Ca2+ Processing by a Unit of Mitochondrial Ca2+ Uniporter and Na+/Ca2+ Exchanger Supports the Neuronal Ca2+ Influx via Activated Glutamate Receptors.
Strokin M1, Reiser G2. Neurochem Res. 2016 Feb 3. [Epub ahead of print]
The current study demonstrates that in hippocampal neurons mitochondrial Ca2+ processing supports Ca2+ influx via ionotropic glutamate (Glu) receptors. We define mitochondrial Ca2+ processing as Ca2+ uptake via mitochondrial Ca2+ uniporter (MCU) combined with subsequent Ca2+ release via mitochondrial Na+/Ca2+ exchanger (NCX). Our tool is to measure the Ca2+ influx rate in primary hippocampal co-cultures, i.e. neurons and astrocytes, by fluorescent digital microscopy, using a Fura-2-quenching method where we add small amounts of Mn2+ in the superfusion medium. Thus, Ca2+ influx is measured with Mn2+ in the bath. Ru360 as inhibitor of mitochondrial Ca2+ uptake through MCU strongly reduces the rate of Ca2+ influx in Glu-stimulated primary hippocampal neurons. Similarly, the Ca2+ influx rate in Glu-stimulated neurons declines after suppression of potential-dependent MCU, when we depolarize mitochondria with rotenone. With inhibition of Ca2+ release from mitochondria via NCX using CGP-37157 the Ca2+ influx via N-methyl-D-aspartate (NMDA)- and kainate-sensitive receptors is slowed down.
3.Reevesioside F induces potent and efficient anti-proliferative and apoptotic activities through Na⁺/K⁺-ATPase α3 subunit-involved mitochondrial stress and amplification of caspase cascades.
Chan SH1, Leu WJ, Hsu LC, Chang HS, Hwang TL, Chen IS, Chen CS, Guh JH. Biochem Pharmacol. 2013 Dec 1;86(11):1564-75. doi: 10.1016/j.bcp.2013.09.021. Epub 2013 Oct 4.
Reevesioside F, isolated from Reevesia formosana, induced anti-proliferative activity that was highly correlated with the expression of Na⁺/K⁺-ATPase α₃ subunit in several cell lines, including human leukemia HL-60 and Jurkat cells, and some other cell lines. Knockdown of α₃ subunit significantly inhibited cell apoptosis suggesting a crucial role of the α₃ subunit. Reevesioside F induced a rapid down-regulation of survivin protein, followed by release of cytochrome c from mitochondria and loss of mitochondrial membrane potential (ΔΨm). Further examination demonstrated the mitochondrial damage in leukemic cells through Mcl-1 down-regulation, Noxa up-regulation and an increase of the formation of truncated Bid, tBim and a 23-kDa cleaved Bcl-2 fragment. Furthermore, reevesioside F induced an increase of mitochondria-associated acetyl α-tubulin that may also contribute to apoptosis. The caspase cascade was profoundly activated by reevesioside F.
4.Pharmacological discrimination of plasmalemmal and mitochondrial sodium-calcium exchanger in cardiomyocyte-derived H9c2 cells.
Namekata I1, Hamaguchi S, Tanaka H. Biol Pharm Bull. 2015;38(1):147-50. doi: 10.1248/bpb.b14-00525.
We examined the effects of SEA0400 and CGP-37157 on the plasmalemmal Na(+)-Ca(2+) exchanger (NCX) and mitochondrial NCX using H9c2 cardiomyocytes loaded with Ca(2+)-sensitive fluorescent probes. The plasmalemmal NCX activity, which was measured as the increase in cytoplasmic Ca(2+) concentration after application of low Na(+) extracellular solution, was inhibited by SEA0400 but not by CGP-37157. The mitochondrial NCX activity, which was measured in permeabilized H9c2 cells as the decrease in mitochondrial Ca(2+) concentration after application of Ca(2+)-free extramitochondrial solution, was inhibited by CGP-37157 but not by SEA0400. These results indicate that SEA0400 and CGP-37157 act as selective inhibitors towards plasmalemmal and mitochondrial NCX, respectively, and provide pharmacological evidence that the plasmalemmal and mitochondrial NCX are distinct molecular entities.
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CAS 75450-34-9 CGP 37157

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