Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 360 nM against mitochondrial Na+/Ca2+ exchanger

Primary TargetMitochondrial Na+/Ca2+ exchanger

Cell permeable: yes

General description

A cell-permeable benzothiazepine derivative of clonazepam that acts as a specific and potent inhibitor of the mitochondrial Na⁺/Ca²⁺ exchanger (IC₅₀ = 360 nM). Enhances the export of Ca²⁺ from isolated mitochondria. Also reported to directly inhibit voltage-gated Ca²⁺ channels.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Jornot, L., et al. 1999. J. Cell Sci.112, 1013.Babcock, D.F., et al. 1997. J. Cell Biol.136, 833.Baron. K.T., and Thayer, S.A. 1997. Eur. J. Pharmacol.340, 295.Griffiths, E.J., et al. 1997. Cell Calcium21, 321.White, R.J., and Reynolds, I.J. 1996, J. Neurosci.16, 5688.Cox, D.A., et al. 1993. J. Cardivasc. Pharmacol.21, 595.Cox, D.A., and Matlib, M.A. 1993. J. Biol. Chem.268, 938.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Preparation Note

Dilute in Ca²⁺-free buffer just prior to use.

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)