Drug intelligence / Profile preview

KB-R7943

Development stage
Preclinical
Lead developer
Nippon Kayaku
Modality
Small Molecules
Administration
Intravenous
01

Overview

KB-R7943 is a small molecule research compound best known as a selective inhibitor of the reverse mode of the sodium-calcium exchanger (NCX), particularly targeting NCX1 with an IC50 of approximately 0.7 μM. It also inhibits the mitochondrial calcium uniporter (MCU) with a Ki of 5.5 μM, and at higher concentrations can partially block NMDA receptor-mediated currents and inhibit mitochondrial respiratory complex I. KB-R7943 is widely used in pharmacological studies investigating calcium homeostasis, neuronal excitotoxicity, cardiac and neuronal injury, and cell death processes. It can induce apoptosis and cell cycle arrest in cancer cell models, and displays cardioprotective and neuroprotective properties under specific experimental conditions. The compound is not approved for clinical or therapeutic use and is intended for laboratory research only[2][4][5][7][9][10].

Other names
KB-R7943 mesylateKB-R-7943 mesylateKB-R 7943 mesylate2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate
02

Targets

NCX1 (Sodium/calcium exchanger 1)NMDAR (Glutamate receptor ionotropic, NMDA)ND1 (Mitochondrial electron transport chain complex I)KCNH2 (Voltage-gated potassium channel subfamily H member 2)MCU (Mitochondrial calcium uniporter)

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