An inhibitor of the reverse Na+/Ca2+ exchanger
Technical Support & Resources

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

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
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
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    5 mg

    $54

    Add

    10 mg

    $85

    Add

    50 mg

    $341

    Add
    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).