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KB-R7943 mesylate

Catalog No. T6144   CAS 182004-65-5
Synonyms: KB-R7943

KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev) with IC50 of 5.7±2.1 μM.

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KB-R7943 mesylate Chemical Structure
KB-R7943 mesylate, CAS 182004-65-5
Pack Size Availability Price/USD Quantity
5 mg In stock $ 50.00
10 mg In stock $ 64.00
25 mg In stock $ 131.00
50 mg In stock $ 236.00
100 mg In stock $ 355.00
1 mL * 10 mM (in DMSO) In stock $ 65.00
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Purity: 99.22%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev) with IC50 of 5.7±2.1 μM.
Targets&IC50 Na+/Ca2+ exchanger:5.7±2.1 µM
In vitro KB-R7943 inhibited NCX(rev) with IC(50) = 5.7 ± 2.1 μM, blocked NMDAR-mediated ion currents, and inhibited NMDA-induced increase in cytosolic Ca(2+) with IC(50) = 13.4 ± 3.6 μM but accelerated calcium deregulation and mitochondrial depolarization in glutamate-treated neurons.?KB-R7943 depolarized mitochondria in a Ca(2+) -independent manner.?Stimulation of NMDA receptors caused NAD(P)H oxidation that was coupled or uncoupled from ATP synthesis depending on the presence of Ca(2+) in the bath solution.?KB-R7943, or rotenone, increased NAD(P)H autofluorescence under resting conditions and suppressed NAD(P)H oxidation following glutamate application.?KB-R7943 inhibited 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC(50) = 11.4 ± 2.4 μM.?With isolated brain mitochondria, KB-R7943 inhibited respiration, depolarized organelles and suppressed Ca(2+) uptake when mitochondria oxidized complex I substrates but was ineffective when mitochondria were supplied with succinate, a complex II substrate[1].
Cell Research Fluorescence microscopy, electrophysiological patch-clamp techniques and cellular respirometry with Seahorse XF24 analyzer were used with cultured hippocampal neurons;?membrane potential imaging, respirometry and Ca(2+) flux measurements were made in isolated rat brain mitochondria[1].
Synonyms KB-R7943
Molecular Weight 427.5
Formula C17H21N3O6S2
CAS No. 182004-65-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27 mg/mL (63.16 mM)

TargetMolReferences and Literature

1. Brustovetsky T , Brittain M K , Sheets P L , et al. KB-R7943, an inhibitor of the reverse Na+ /Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I.[J]. British Journal of Pharmacology, 2015, 162(1):255-270. 2. Barrientos G , Bose D D , Feng W , et al. The Na+/Ca2+ Exchange Inhibitor 2-(2-(4-(4-Nitrobenzyloxy)phenyl)ethyl)isothiourea Methanesulfonate (KB-R7943) Also Blocks Ryanodine Receptors Type 1 (RyR1) and Type 2 (RyR2) Channels[J]. Molecular Pharmacology, 2009, 76(3):560-568.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Sodium Channel Blocker Library Inhibitor Library Autophagy Compound Library Bioactive Compound Library Anti-Cancer Compound Library NO PAINS Compound Library Ion Channel Inhibitor Library Bioactive Compounds Library Max

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Keywords

KB-R7943 mesylate 182004-65-5 Autophagy Membrane transporter/Ion channel Na+/Ca2+ Exchanger KB-R7943 inhibit KB-R 7943 Mesylate KB-R-7943 mesylate KB-R 7943 KB-R7943 Mesylate Inhibitor KB-R-7943 Mesylate KB R7943 mesylate KBR7943 mesylate KB-R-7943 inhibitor

 

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