| CAS NO: | 1154-25-2 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 299.76 |
| Cas No. | 1154-25-2 |
| Formula | C11H8ClN7O |
| Solubility | Soluble in DMSO |
| Chemical Name | 3-amino-6-chloro-N-(diaminomethylene)-5-(ethyl(isopropyl)amino)pyrazine-2-carboxamide |
| Canonical SMILES | ClC1=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 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。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。 |
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.
| 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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