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YM-244769
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图片
CAS NO:838819-70-8
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 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 优先抑制NCX3,抑制 NCX 单向向外电流 (Ca2+进入模式),IC50值分别为 18 nM 和 50 nM。YM-244769 可有效预防缺氧/复氧诱导的 SH-SY5Y 神经元细胞损伤。YM-244769 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 is a potent, selective and orally active Na+/Ca2+exchanger (NCX) inhibitor. YM-244769 preferentially inhibitsNCX3and suppresses the unidirectional outward NCX current (Ca2+entry mode), withIC50s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice[1][2][3].

IC50& Target

IC50: 18 nM (NCX3), 68 nM (NCX1), 96 nM (NCX2)[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].

Cell Viability Assay[1]

Cell Line:SH-SY5Y cells treated with NCX1 or NCX3 antisense
Concentration:0.3 and 1 μM
Incubation Time:
Result:Hypoxia/reoxygenation-induced LDH release was significantly attenuated: reduction in cell damage was greater in cells treated with NCX3 antisense (by 61%) than in cells treated with NCX1 antisense (by 35%). 0.3 or 1 μM efficiently suppressed the hypoxia/reoxygenation-induced cell damage in SH-SY5Y cells treated with NCX1 antisense more than in those treated with NCX3 antisense.
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 increases 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

443.47

性状

Solid

Formula

C26H22FN3O3

CAS 号

838819-70-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 120 mg/mL(270.59 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.2549 mL11.2747 mL22.5494 mL
5 mM0.4510 mL2.2549 mL4.5099 mL
10 mM0.2255 mL1.1275 mL2.2549 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (4.69 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.69 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。