MDL | MFCD00952138 |
---|---|
Molecular Weight | 427.50 |
Molecular Formula | C17H21N3O6S2 |
SMILES | NC(SCCC1=CC=C(OCC2=CC=C([N+]([O-])=O)C=C2)C=C1)=N.CS(=O)(O)=O |
IC50: 5.7±2.1 µM (Na + /Ca 2+ exchanger) [1]
KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca 2+ with IC 50 =13.4±3.6 µM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca 2+ -independent manner. KB-R7943 inhibits 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC 50 =11.4±2.4 µM. In addition to NCX rev , KB-R7943 dose-dependently and reversibly blocked ion currents elicited by NMDA. KB-R7943 dose-dependently inhibits NMDA-induced increases in [Ca 2+ ] c with IC 50 =13.4±3.6 µM confirming the inhibition of NMDA receptors observed in electrophysiological experiments [1] . wt RyR1-HEK 293 pretreated with KB-R7943 (10 μM, 10 min) dissolved in the bulk perfusion exhibited significantly attenuated responses to caffeine. In this regard, KB-R7943 produced more pronounced inhibition of caffeine-induced Ca 2+ release elicited by 1 mM compared with 0.5 and 0.75 mM (60 versus 58 versus 37%, p<0.05, respectively) [2] . KB-R7943 inhibits both I hERG and native I Kr rapidly on membrane depolarization with IC 50 values of ~89 and ~120 nM, respectively, for current tails at −40 mV following depolarizing voltage commands to +20 mV. I hERG inhibition by KB-R7943 exhibits both time- and voltage-dependence but shows no preference for inactivated over activated channels [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solid
Room temperature in continental US; may vary elsewhere.
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
DMSO : 100 mg/mL ( 233.92 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 2.3392 mL | 11.6959 mL | 23.3918 mL |
5 mM | 0.4678 mL | 2.3392 mL | 4.6784 mL |
10 mM | 0.2339 mL | 1.1696 mL | 2.3392 mL |