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KB-R7943 mesylate

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Catalog No. T6144Cas No. 182004-65-5

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

KB-R7943 mesylate

KB-R7943 mesylate

🥰Excellent
Purity: 99.22%
Catalog No. T6144Cas No. 182004-65-5
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 SizePriceAvailabilityQuantity
5 mg$50In Stock
10 mg$64In Stock
25 mg$131In Stock
50 mg$236In Stock
100 mg$355In Stock
1 mL x 10 mM (in DMSO)$65In Stock
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Purity:99.22%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight427.5
FormulaC17H21N3O6S2
Cas No.182004-65-5
SmilesCS(O)(=O)=O.NC(=N)SCCc1ccc(OCc2ccc(cc2)[N+]([O-])=O)cc1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.3392 mL11.6959 mL23.3918 mL116.9591 mL
5 mM0.4678 mL2.3392 mL4.6784 mL23.3918 mL
10 mM0.2339 mL1.1696 mL2.3392 mL11.6959 mL
20 mM0.1170 mL0.5848 mL1.1696 mL5.8480 mL
50 mM0.0468 mL0.2339 mL0.4678 mL2.3392 mL
100 mM0.0234 mL0.1170 mL0.2339 mL1.1696 mL

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