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EIPA is a TRPP3 channel inhibitor with an IC50 value of 10.5 μM, EIPA also inhibits Sodium-hydrogen exchangers (NHE) and macropinocytosis[1].
In Chinese hamster ovary cells, EIPA is a Na+/Ca2+ exchange (NCX) inhibitor that inhibits ET-1-induced continuous increase of intracellular Ca2+ concentration. In Xenopus oocytes, EIPA can rapidly and reversibly block calcium ion-activated TRPP3 channel activation at -50mV and other membrane potentials[2].
References:
[1]. Dai X Q, et al. Inhibition of TRPP3 channel by MK-870 and analogs. Mol Pharmacol, 2007, 72(6): 1576-85.
[2]. Horinouchi T, Miyake Y, Nishiya T, et al. Functional Role of Na+/H+ Exchanger in Ca2+ Influx Mediated via Human Endothelin Type A Receptor Stably Expressed in Chinese Hamster Ovary Cells. Journal of Pharmacological Sciences, 2008, 107(4): 456-459.
Cell lines
Chinese hamster ovary cells ; X. laevis oocytes expressed TRPP3
Preparation method
The solubility of this compound in DMSO is >10mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition
Chinese hamster ovary cells were treated with 10 μM EIPA for 30 minOocytes were treated with 100μM EIPA.
Applications
In chinese hamster ovary Cells, EIPA ,a Na+/Ca2+ exchanger (NCX) inhibitor, inhibited ET-1-induced sustained increases in intracellular Ca2+ concentration ([Ca2+]i).In X. laevis oocytes, EIPA rapidly and reversibly blocked Ca2+ activated TRPP3 channel activation at -50 mV as well as at other membrane potentials.
[1] .Dai et al (2007) Inhibition of TRPP3 channel by amiloride and analogs. Mol.Pharmacol. 72 1576. PMID: 17804601.
[2]. Horinouchi et al (2008) Functional role of Na+/H+ exchanger in Ca2+ influx mediated via human endothelin type A receptor stably expressed in Chinese hamster ovary cells. J.Pharm.Sci. 107 456. PMID: 18678984.
