A selective inhibitor of the reverse mode of NCX1 (IC50 = 1.2-2.4 µM) that prevents intracellular sodium-dependent calcium uptake in whole cells; exhibits neuroprotection from glutamate-induced excitotoxicity; inhibits TRPC channels involved in calcium-dependent signal transduction

KB-R7943 (mesylate) – 50 mg

Brand:
Cayman
CAS:
182004-65-5
Storage:
-20
UN-No:
Non-Hazardous - /

The Na+/Ca2+ exchanger (NCX) is a major regulator of intracellular calcium concentration that is largely expressed in cardiac sarcolemma (NCX1) but also in brain and skeletal muscle (NCX2). KB-R7943 is an isothiourea derivative that selectively inhibits the reverse mode of NCX1 (IC50 = 1.2-2.4 µM), preventing intracellular sodium-dependent calcium uptake in whole cells.{26636} It is much less potent at preventing extracellular sodium-dependent calcium efflux from intact cells (IC50 > 30 µM).{26636} In cultured hippocampal neurons, KB-R7943 exhibits neuroprotection from glutamate-induced excitotoxicity by blocking NMDA receptor-mediated activity (IC50 = 13.4 µM) and inhibiting complex I in the mitochondrial respiratory chain (IC50 = 11.4 µM).{26637} KB-R7943 has also been shown to block transient receptor potential canonical channels, which are important mediators of calcium-dependent signal transduction.{26638}  

 

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Description

A selective inhibitor of the reverse mode of NCX1 (IC50 = 1.2-2.4 µM) that prevents intracellular sodium-dependent calcium uptake in whole cells; exhibits neuroprotection from glutamate-induced excitotoxicity; inhibits TRPC channels involved in calcium-dependent signal transduction

Formal name: 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester carbamimidothioic acid, monomethanesulfonate

Synonyms: 

Molecular weight: 427.5

CAS: 182004-65-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cell Biology|Cell Signaling|Calcium Mobilization||Research Area|Cell Biology|Mitochondrial Biology||Research Area|Neuroscience

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