General description
A cell-permeable inhibitor of the influx/reverse mode of the Na+/Ca2+ exchanger (NCX) (IC50 = 4.3 µM for NCX1, 4.7 µM for NCX2, and 1.4 µM for NCX3). Directly modulates Na+/Mg2+ exchange in a Ca2+-dependent manner. Reported ot offer neuronal and cardio-protection against ischemic injury. Also inhibits nicotinic acetylcholine receptors and NMDA receptor channels (IC50<10 µM).
A cell-permeable isothiourea derivative that inhibits the influx/reverse mode of Na+/Ca2+ exchangers (NCX; IC50 = 4.3 µM, 4.7 µM, and 1.4 µM for NCX1,NCX2, and NCX3, respectively) and directly modulates Na+/Mg2+ exchange in a Ca2+-dependent manner. Reported to offer neuronal and cardioprotection. Also inhibits nicotinic acetylcholine receptors and NMDA receptor channels (IC50<10 µM).
Biochem/physiol Actions
Primary Target
Na+/Ca2+ exchangers
Target IC50: 4.3 µM, 4.7 µM, and 1.4 µM for NCX1,NCX2, and NCX3, respectively
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Hobai, I.A., and O′Rourke, B. 2004. Expert Opin. Investig. Drugs13, 653.
Uetani, T., et al. 2003. J. Biol. Chem.278, 47491.
Iwamoto, T., et al. 2001. Mol. Pharmacol.59, 524.
Pintado, A.J., et al. 2000. Br. J. Pharmacol.130, 1893.
Sobolevsky, A.I., and Khodorov, B.I. 1999. Neuropharmacology38, 1235.
Iwamoto, T., et al. 1996. J. Biol. Chem.271, 22391.
Watano, T., et al. 1996. Br. J. Pharmacol.119, 555.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51141595
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 420336-5MG
- CAS:
- 182004-65-5