KB-R7943 (mesylate)

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KB-R7943 (mesylate)

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Cat No: 16352

Biochemicals - Transporter & Exchanger Modulators

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 inhibit...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

182004-64-4 inhibitors inhibits inhibitions NCX1 Na+/Ca2+ sodium/calcium Na+ Ca2+ exchangers sodium calcium neuroprotection TRPC signals transduction mesylate KBR7943 KB R7943 KB-R 7943 R reverse NCX isothiourea derivatives selective selectively sodium-dependent dependent neurons NMDA receptors complex I 1 one mitochondria mitochondrial respiratory chains transient potential canonical channels cardiology ions pumps blockers biology neurosciences

Product Overview:
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}

Size	5 mg
Shipping	dry ice
CAS Number	182004-65-5
Molecular Formula	C₁₆H₁₇N₃O₃S • CH₃SO₃H
SMILES	NC(SCCC(C=C1)=CC=C1OCC2=CC=C([N+]([O-])=O)C=C2)=N.OS(C)(=O)=O
Molecular Weight	427,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2930.90
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.