An inhibitor of the reverse Na+/Ca2+ exchanger
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KB-R7943 (mesylate)

Item No. 16352

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
carbamimidothioic acid, 2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl ester, monomethanesulfonate
CAS Number
182004-65-5
Molecular Formula
C16H17N3O3S • CH3SO3H
Formula Weight
427.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
223, 269 nm
SMILES
NC(SCCC(C=C1)=CC=C1OCC2=CC=C([N+]([O-])=O)C=C2)=N.OS(C)(=O)=O
InChi Code
InChI=1S/C16H17N3O3S.CH4O3S/c17-16(18)23-10-9-12-3-7-15(8-4-12)22-11-13-1-5-14(6-2-13)19(20)21;1-5(2,3)4/h1-8H,9-11H2,(H3,17,18);1H3,(H,2,3,4)
InChi Key
WGIKEBHIKKWJLG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $54

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    10 mg

    $85

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    50 mg

    $341

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    Product Description

    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.1 It is much less potent at preventing extracellular sodium-dependent calcium efflux from intact cells (IC50 > 30 µM).1 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).2 KB-R7943 has also been shown to block transient receptor potential canonical channels, which are important mediators of calcium-dependent signal transduction.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Iwamoto, T., Watano, T., and Shigekawa, M. A novel isothiourea derivative selectively inhibits the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1. The Journal of Biological Chemisty 271(37), 22391-22397 (1996).

    2. Brustovetsky, T., Brittain, M.K., Sheets, P.L., et al. KB-R7943, an inhibitor of the reverse Na+/Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I. Br. J. Pharmacol. 162(1), 255-270 (2011).

    3. Wu, X., Eder, P., Chang, B., et al. TRPC channels are necessary mediators of pathologic cardiac hypertrophy. Proc. Natl. Acad. Sci. USA 107(15), 7000-7005 (2010).