YM-244769

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Chemical Structure| 838819-70-8 同义名 : -
CAS号 : 838819-70-8
货号 : A1671514
分子式 : C26H22FN3O3
纯度 : 99%+
分子量 : 443.47
MDL号 : MFCD28160863
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 115 mg/mL(259.32 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 YM-244769 is a potent, selective, and orally active inhibitor of the Na+/Ca2+ exchanger (NCX). It preferentially targets NCX3 and inhibits the unidirectional outward NCX current (Ca2+ entry mode) with IC50 values of 18 nM and 50 nM, respectively. YM-244769 effectively guards against hypoxia/reoxygenation-induced damage in SH-SY5Y neuronal cells. Additionally, it increases urine volume and the urinary excretion of electrolytes in mice [1][2][3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.23mL

11.27mL

2.25mL

1.13mL

22.55mL

4.51mL

2.25mL
参考文献

[1]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.

[2]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.

[3]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.