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EIPA

 
Catalog No.
B7389
TRPP3通道抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,083.00
Ship with 10-15 days
10mg
¥ 2,058.00
Ship with 10-15 days
25mg
¥ 3,033.00
Ship with 10-15 days

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A

背景

EIPA is a TRPP3 channel inhibitor with an IC50 value of 10.5 μM, EIPA also inhibits Sodium-hydrogen exchangers (NHE) and macropinocytosis[1].

In Chinese hamster ovary cells, EIPA is a Na+/Ca2+ exchange (NCX) inhibitor that inhibits ET-1-induced continuous increase of intracellular Ca2+ concentration. In Xenopus oocytes, EIPA can rapidly and reversibly block calcium ion-activated TRPP3 channel activation at -50mV and other membrane potentials[2].

References:

[1]. Dai X Q, et al. Inhibition of TRPP3 channel by MK-870 and analogs. Mol Pharmacol, 2007, 72(6): 1576-85.

[2]. Horinouchi T, Miyake Y, Nishiya T, et al. Functional Role of Na+/H+ Exchanger in Ca2+ Influx Mediated via Human Endothelin Type A Receptor Stably Expressed in Chinese Hamster Ovary Cells. Journal of Pharmacological Sciences, 2008, 107(4): 456-459.

文献引用

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt299.76
Cas No.1154-25-2
FormulaC11H8ClN7O
SolubilitySoluble in DMSO
Chemical Name3-amino-6-chloro-N-(diaminomethylene)-5-(ethyl(isopropyl)amino)pyrazine-2-carboxamide
SDFDownload SDF
Canonical SMILESClC1=NC(C(/N=C(N)\N)=O)=C(N)N=C1N(CC)C(C)C
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

试验操作

细胞实验[1]:

细胞系

中国仓鼠卵巢细胞; 表达TRPP3的非洲爪蟾卵母细胞

溶解方法

在DMSO中的溶解度>10mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

中国仓鼠卵巢细胞用10μM EIPA处理30分钟; 用100 μM EIPA处理非洲爪蟾卵母细胞

应用

在中国仓鼠卵巢细胞中,EIPA是一个Na+/Ca2+ 交换(NCX)抑制剂,抑制ET-1诱导的细胞内Ca2+ 浓度持续增加([Ca2+]i)。在非洲爪蟾卵母细胞中,EIPA在-50mV以及其他膜电位下能够快速且可逆地阻断Ca2+激活的TRPP3通道活化。

References:

[1] .Dai et al (2007) Inhibition of TRPP3 channel by amiloride and analogs. Mol.Pharmacol. 72 1576. PMID: 17804601.

[2]. Horinouchi et al (2008) Functional role of Na+/H+ exchanger in Ca2+ influx mediated via human endothelin type A receptor stably expressed in Chinese hamster ovary cells. J.Pharm.Sci. 107 456. PMID: 18678984.

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