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EIPA 目录号 GC15893

TRPP3 channel inhibitor

规格 价格 库存 购买数量
10mg
¥714.00
现货
50mg
¥2,877.00
现货

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Sample solution is provided at 25 µL, 10mM.

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质量管理

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

Chinese hamster ovary cells ; X. laevis oocytes expressed TRPP3

Preparation method

The solubility of this compound in DMSO is >10mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

Chinese hamster ovary cells were treated with 10 μM EIPA for 30 minOocytes were treated with 100μM EIPA.

Applications

In chinese hamster ovary Cells, EIPA ,a Na+/Ca2+ exchanger (NCX) inhibitor, inhibited ET-1-induced sustained increases in intracellular Ca2+ concentration ([Ca2+]i).In X. laevis oocytes, EIPA rapidly and reversibly blocked Ca2+ activated TRPP3 channel activation at -50 mV as well as at other membrane potentials.

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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Chemical Properties

Cas No. 1154-25-2 SDF
别名 N/A
化学名 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
分子式 C11H8ClN7O 分子量 299.76
溶解度 Soluble in DMSO 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

Sodium-hydrogen exchangers (NHE) are involved in maintaining sodium and pH balance in a variety of tissues. They are also known as sodium-hydrogen antiporters and solute carrier family 9 members. 5-(N-ethyl-N-isopropyl)-Amiloride (EIPA) is a potent inhibitor of several NHE isoforms, inhibiting NHE1, NHE2, NHE3, and NHE5 with Ki values of 0.02, 0.5, 2.4, and 0.42 μM, respectively[1],[2] It less effectively inhibits NHE4 (IC50 ≥10 μM).[1] EIPA is commonly used at a concentration of 5-10 μM to inhibit cellular HNE activity.[3],[4]


Reference:
[1]. Masereel, B., Pochet, L., and Laeckmann, D. An overview of inhibitors of Na+/H+ exchanger Eur. J. Med. Chem. 38(6), 547-554 (2003).
[2]. Attaphitaya, S., Park, K., and Melvin, J.E. Molecular cloning and functional expression of a rat Na+/H+ exchanger (NHE5) highly expressed in brain The Journal of Biological Chemisty 274(7), 4383-4388 (1999).
[3]. Hwang, S.M., Koo, N.Y., Jin, M., et al. Intracellular acidification is associated with changes in free cytosolic calcium and inhibition of action potentials in rat trigeminal ganglion The Journal of Biological Chemisty 286(3), 1719-1729 (2011).[4]. Xue, L., Aihara, E., Wang, T.C., et al. Trefoil factor 2 requires Na/H exchanger 2 activity to enhance mouse gastric epithelial repair The Journal of Biological Chemisty 286(44), 38375-38382 (2011).