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KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev), with an IC50 of 5.7±2.1 μM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $50 | In Stock | |
10 mg | $64 | In Stock | |
25 mg | $131 | In Stock | |
50 mg | $236 | In Stock | |
100 mg | $355 | In Stock | |
1 mL x 10 mM (in DMSO) | $65 | In Stock |
Description | KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev), with an 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]. |
Molecular Weight | 427.5 |
Formula | C17H21N3O6S2 |
Cas No. | 182004-65-5 |
Smiles | CS(O)(=O)=O.NC(=N)SCCc1ccc(OCc2ccc(cc2)[N+]([O-])=O)cc1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (128.65 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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