KB-R7943

SKU: orb1220619

Description

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

Key Properties

• CAS Number: 182004-65-5
• MW: 427.5
• Purity: >98% (HPLC)
• Formula: C₁₇H₂₁N₃O₆S₂
• SMILES: CS(O)(=O)=O.NC(=N)SCCc1ccc(OCc2ccc(cc2)[N+]([O-])=O)cc1
• Target: Na+/Ca2+ Exchanger
• Solubility: DMSO:27 mg/mL (63.16 mM)

Bioactivity

• In Vitro:
  KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca2+ with IC50 = 13.4 ± 3.6 μM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca2+-independent manner. KB-R7943 inhibits 2, 4-dinitrophenol-stimulated respiration of cultured neurons with IC50 = 11.4 ± 2.4 μM. In addition to NCXrev, KB-R7943 dose-dependently and reversibly blocked ion currents elicited by NMDA. KB-R7943 dose-dependently inhibits NMDA-induced increases in [Ca2+]c with IC50 = 13.4 ± 3.6 μM confirming the inhibition of NMDA receptors observed in electrophysiological experiments. wtRyR1-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 Ca2+ release elicited by 1 mM compared with 0.5 and 0.75 mM (60 versus 58 versus 37%, p< 0.05, respectively). KB-R7943 inhibits both IhERG and native IKr rapidly on membrane depolarization with IC50 values of ~89 and ~120 nM, respectively, for current tails at 40 mV following depolarizing voltage commands to +20 mV. IhERG inhibition by KB-R7943 exhibits both time- and voltage-dependence but shows no preference for inactivated over activated channels.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KB-R7943 mesylate

Quick Database Links

Gene Symbol

Na+/Ca2+ Exchanger