YM-244769 hydrochloride is a potent, selective and orally active Na⁺/Ca²⁺ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca²⁺ entry mode), with IC₅₀s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice.

YM-244769 (0.003-1 μM) inhibits dose dependently 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.
YM-244769 (0.3 or 1 μM) efficiently protects against the hypoxia/reoxygenation-induced lactate dehydrogenase (LDH) release in SH-SY5Y cells and in LLC-PK₁ cells (1 μM).
YM-244769 possesses reverse mode-selectivity.
YM-244769 (1 and 10 μM) inhibits NCX current (I_NCX) in a concentration- and [Na⁺]_i-dependent manner, the IC₅₀ against the unidirectional outward I_NCX (Ca²⁺ entry mode) is 0.05 μM. The IC₅₀ values against the bidirectional outward and inward I_NCX are similar and approximately 100 nM with a Hill coefficient of about 1.
YM-244769 is trypsin-insensitive.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

YM-244769 (0.1-1 mg/kg; p.o.; once) exhibits dose-dependently natriuretic action in mice and significantly increased urinary excretion of Ca²⁺ as well as Ca²⁺/Cr ratio.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

YM-244769 (0.1-1 mg/kg; p.o.; once) exhibits dose-dependently natriuretic action in mice and significantly increased urinary excretion of Ca²⁺ as well as Ca²⁺/Cr ratio.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Iwamoto T, Kita S. YM-244769, a novel Na+/Ca2+ exchange inhibitor that preferentially inhibits NCX3, efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. Mol Pharmacol. 2006 Dec;70(6):2075-83.  [Content Brief]

  . Gotoh Y, et al. Genetic knockout and pharmacologic inhibition of NCX2 cause natriuresis and hypercalciuria. Biochem Biophys Res Commun. 2015 Jan 9;456(2):670-5.  [Content Brief]

  . Yamashita K, et al. Inhibitory effect of YM-244769, a novel Na+/Ca2+ exchanger inhibitor on Na+/Ca2+ exchange current in guinea pig cardiac ventricular myocytes. Naunyn Schmiedebergs Arch Pharmacol. 2016 Nov;389(11):1205-1214.  [Content Brief]