Biological Activity |
SN 6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor, and inhibits 45Ca2+ uptake by NCX1, NCX2, and NCX3, with IC50s of 2.9, 16, and 8.6 uM, respectively. IC50 & Target: IC50:2.9 uM (NCX1), 16 uM (NCX2), 8.6 uM (NCX3)[1] In Vitro: SN 6 is a selective Na+/Ca2+ exchanger inhibitor, which inhibits the initial rate of 45Ca2+ uptake into NCX1, NCX2, and NCX3 transfectants with IC50 values of 2.9 +/- 0.12, 16 +/- 1.1, and 8.6 +/- 0.27 uM. SN 6 (up to 30 uM) also less potently inhibits muscarinic acetylcholine receptor, with a higher IC50 of 18 uM. SN 6 (0.3-30 uM) completely inhibits the initial rate of Na+i-dependent 45Ca2+ uptake into Na+-loaded sarcolemmal vesicles in a dose dependent manner (IC50, 5.3 +/- 0.37 uM). SN 6 (0.3-10 uM) dose-dependently protects against the hypoxia/reoxygenation-induced LDH release in parental LLC-PK1 cells and NCX1 transfectants but not in K229Q transfectants[1]. SN 6 (1-30 uM) suppresses the bidirectional outward and inward INCX in a concentration-dependent manner, with IC50 values of 2.3 uM and 1.9 uM, respectively. SN 6 also inhibits bidirectional current (INCX) in a [Na+]i concentration-dependent manner, with IC50 values of 3.4 uM, 2.3 uM, and 1.1 uM at 10 mM, 20 mM, and 30 mM [Na+]i, respectively[2]. SN 6 inhibits hypoxia/reoxygenation-induced LDH release with an IC50 value of 0.63 +/- 0.15 uM in NCX1 transfectants[3]. |