YM-244769 dihydrochloride is a potent, selective, and orally active inhibitor of the Na+/Ca2+ exchanger (NCX). It exhibits a preference for inhibiting NCX3 and attenuates the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. Additionally, YM-244769 dihydrochloride effectively protects against hypoxia/reoxygenation-induced damage in SH-SY5Y neuronal cells. Moreover, it can enhance urine volume and urinary electrolyte excretion in mice [1][2][3].
体内研究
YM-244769 (0.1-1 mg/kg; pO.; once) demonstrates a dose-dependent natriuretic effect in mice. Additionally, it significantly enhances urinary excretion of Ca2+ as well as Ca2+/Cr ratio[2].
体外研究
YM-244769 (0.003-1 μM) dose-dependently inhibits the initial rates of 45Ca2+ uptake into NCX1, NCX2, and NCX3 transfectants, with IC50 values of 68 ± 2.9, 96 ± 3.5, and 18 ± 1.0 nM, respectively [1].
YM-244769 (0.3 or 1 μM) effectively prevents hypoxia/reoxygenation-induced lactate dehydrogenase (LDH) release in SH-SY5Y cells and LLC-PK1 cells (at 1 μM) [1].
YM-244769 exhibits selectivity for the reverse mode [1].
YM-244769 (1 and 10 μM) demonstrates inhibition of the NCX current (INCX) in a manner dependent on both concentration and intracellular sodium concentration ([Na+]i). The half-maximal inhibitory concentration (IC50) against the unidirectional outward INCX (Ca2+ entry mode) is 0.05 μM. The IC50 values for both bidirectional outward and inward INCX are approximately 100 nM, with a Hill coefficient of approximately 1.
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