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YM 244769

Na+/Ca2+交换（NCX）反向模式的抑制剂

目录号: PC12028 纯度: ≥98%

CAS No. :837424-39-2

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中文名称

YM 244769

英文名称

YM 244769

英文别名

YM 2447690;N-(3-Aminobenzyl)-6-{4-[(3-fluorobenzyl)oxy]phenoxy}nicotinamide dihydrochloride;YM 244769

Cas No.

837424-39-2

分子式

C₂₆H₂₂N₃O₃F^.₂[HCl]

分子量

516.39

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

YM-244769 hydrochloride is a potent, selective and orally active Na/Ca exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 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.

性状

Solid

IC50 & Target[1][2]

IC₅₀: 18 nM (NCX3)

体外研究(In Vitro)

YM-244769 (0.003-1 μM) inhibits dose dependently the initial rates of Ca 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 (Ca 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.

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

体内研究(In Vivo)

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

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

Animal Model:	Wild-type C57BL/6J mice and NCX-KO mice
Dosage:	0.1, 0.3 and 1 mg/kg
Administration:	Oral administration, once
Result:	Caused a dose-dependent increase (up to approximately 200%) in urine volume and urinary excretion of electrolytes (Na, K and Cl). Natriuretic actions were equivalently observed in NCX1-KO and WT, but disappeared in NCX2-KO and double KO.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

[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. [Information]

[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. [Information]

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Data Sheet

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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