货号	规格	价格	上海	北京	珠海	重庆	武汉
S89814-5mg买3赠1	98.50%	￥710.00 S89814-5mg ￥710.00 现货（买3赠1）	6 6	-	-	-	-
S89814-10mg促销	98.50%	￥1120.00 ￥896.00 S89814-10mg ￥896.00 现货	6 6	-	-	-	-
S89814-25mg促销	98.50%	￥2400.00 ￥1920.00 S89814-25mg ￥1920.00 现货	5 5	-	-	-	-

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产品描述：

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

靶点：

IC50: 18 nM (NCX3), 68 nM (NCX1), 96 nM (NCX2);CalciumChannel

体内研究：

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

参考文献：

1. Takahiro Iwamoto , et al. 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- 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.

溶解性：

Soluble in DMSO

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.937 ml	9.683 ml	19.365 ml
5 mM	0.387 ml	1.937 ml	3.873 ml
10 mM	0.194 ml	0.968 ml	1.937 ml
50 mM	0.039 ml	0.194 ml	0.387 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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计算重置

YM244769.HCl