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YM-244769 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
YM-244769 hydrochloride图片
CAS NO:837424-39-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品介绍
YM-244769 hydrochloride 是一种有效的、选择性的、具有口服活性的 Na+/Ca2+交换体 (NCX) 抑制剂。YM-244769 hydrochloride 优先抑制NCX3,抑制 NCX 单向向外电流 (Ca2+进入模式),IC50分别为 18 nM 和 50 nM。YM-244769 hydrochloride 可有效预防缺氧/复氧诱导的 SH-SY5Y 神经元细胞损伤。YM-244769 hydrochloride 还能增加小鼠的尿量和尿液中电解质的排泄。
生物活性

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), withIC50s 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[1][2][3].

IC50& Target

IC50: 18 nM (NCX3)[1]

体外研究
(In Vitro)

YM-244769 (0.003-1 μM) inhibits dose dependently the initial rates of45Ca2+uptake into NCX1, NCX2, and NCX3 transfectants with IC50values of 68 ± 2.9, 96 ± 3.5, and 18 ± 1.0 nM, respectively[1].
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-PK1cells (1 μM)[1].
YM-244769 possesses reverse mode-selectivity[1].
YM-244769 (1 and 10 μM) inhibits NCX current (INCX) in a concentration- and [Na+]i-dependent manner, the IC50against the unidirectional outward INCX(Ca2+entry mode) is 0.05 μM. The IC50values against the bidirectional outward and inward INCXare similar and approximately 100 nM with a Hill coefficient of about 1[3].
YM-244769 is trypsin-insensitive[3].

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 Ca2+as well as Ca2+/Cr ratio[2].

Animal Model:Wild-type C57BL/6J mice and NCX-KO mice[2]
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.
分子量

479.93

性状

Solid

Formula

C26H23ClFN3O3

CAS 号

837424-39-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month