KB-R7943 mesylate

SKU: orb1301037

Description

KB-R7943 mesylate is a selective inhibitor of the reverse mode sodium-calcium exchanger (NCXrev) with an IC50 of 5.7±2.1 μM. It is widely used in cardiovascular and neurological research to investigate ischemia-reperfusion injury, calcium overload, and related cellular pathways in both in vitro and in vivo models.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 182004-65-5
• MW: 427.49
• Purity: >98%
• Formula: C₁₆H₁₇N₃O₃S ∙ CH₃SO₃H
• SMILES: CS(O)(=O)=O.NC(=N)SCCc1ccc(OCc2ccc(cc2)[N+]([O-])=O)cc1
• Target: Ion channel
• Solubility: Soluble in DMSO (up to 50 mg/ml).

Bioactivity

• Target 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.
• 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.

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, Ca2+ Exchanger, Ca2+Exchanger, KB R7943 mesylate, KB-R 7943, KB-R 7943 Mesylate, KB-R-7943, KBR7943 mesylate, KB-R7943 Mesylate, Na+Exchanger, Na+/Ca2+ Exchanger, Na+ Exchanger

Compound Identifiers

PubChem CID

9823846