EIPA (Synonyms: L-593,754, MH 12-43, 5-(N-ethyl-N-isopropyl)-Amiloride) |
Catalog No.GC15893
One-Click Copy Product Info
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EIPA inhibited TRPP3-mediated Ca2+-activated currents with IC50 values of 10.5 µM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1154-25-2
Sample solution is provided at 25 µL, 10mM.
EIPA inhibited TRPP3-mediated Ca2+-activated currents with IC50 values of 10.5 µM [1]. TRPP3, a member of the transient receptor potential (TRP) superfamily of cation channels, is a Ca2+-activated channel permeable to Ca2+, Na+, and K+ [1].EIPA (5-(N-ethyl-N-isopropyl)-amiloride) is a commonly used amiloride derivative modified similarly to MPA, and its Ki for NHE1, NHE2, and NHE3 are 0.3, 1.8, and 67 µM, respectively[2,3]
EIPA suppressed proliferation of MKN28 cells through up-regulation of p21 expression via reduction of [Cl- ] c as a result from DIDS-sensitive Cl- /HCO3- exchanger-mediated compensation for keeping pHc normal under an NHE-inhibited condition [4].
EIPA preischemic treatment overcame the I/R-induced renal dysfunction. Histologic examination of the kidney of vehicle-treated ARF mice revealed severe lesions, and these lesions were significantly suppressed by the preischemic treatment with EIPA. In addition, EIPA suppressed the increment of renal ET-1 content after reperfusion [5]. EIPA at doses of 3 and 9 mg/kg per day inhibited tumor growth of HepG2 modle mice significantly compared with the control [6].
References:
[1]. Dai XQ, Ramji A, Liu Y, Li Q, Karpinski E, Chen XZ (2007) Inhibition of TRPP3 channel by amiloride and analogs. Mol Pharmacol 72:1576-1585
[2]. Guffey, S.C.; Fliegel, L.; Goss, G.G. Cloning and characterization Na+/H+ Exchanger isoforms, NHE2 and, NHE3 from the gill Pacific dogfish, Squalus suckleyi. Comp. Biochem. Physiol. Part B Biochem. Mol. Biol. 2015, 188, 46-53.
[3]. Masereel, B. An overview inhibitors Na+/H+ exchanger. Eur. J. Med. Chem. 2003, 38, 547-554.
[4]. Hosogi SMH, Nakajima K, Ashihara E, Niisato N, Kusuzaki K, Marunaka Y: An inhibitor of Na(+)/H(+) exchanger (NHE), ethyl-isopropyl amiloride (EIPA), diminishes proliferation of MKN28 human gastric cancer cells by decreasing the cytosolic Cl(-) concentration via DIDS-sensitive pathways. Cell Physiol Biochem. 2012, 30: 1241-1253. 10.1159/000343315.
[5]. Yamashita J, Ohkita M, Takaoka M, Kaneshiro Y, Matsuo T,Kaneko K, Matsumura Y.Role of Na+/H+ exchanger in the pathogen-esis of ischemic acute renal failure in mice.J Cardiovasc Pharmacol49:154 -160, 2007.
[6]. X. Yang, D. Wang, W. Dong, Z. Song, K. Dou.Expression and modulation of Na+/H+ exchanger 1 gene in hepatocellular carcinoma: a potential therapeutic target. J. Gastroenterol. Hepatol., 26 (2) (2011), pp. 364-370
| Cell experiment [1]: | |
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Cell lines |
MCF-7 cells |
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Preparation Method |
Cells were seeded in 6-well plates for 24 h prior to 48 h-treatment with EIPA (10 µM), Akti (1 µM), U0126 (10 µM) or a combination thereof. |
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Reaction Conditions |
10µM for 48 hours |
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Applications |
MCF-7 cells were subjected to treatment with EIPA with and without ERK and Akt inhibitors. ERK, but not Akt, activity was increased upon EIPA treatment, and both kinases were effectively inhibited by their inhibitors, U0126 and Akti, respectively. Strikingly, ERK inhibition strongly potentiated EIPA-induced CHOP upregulation and PARP cleavage. |
| Animal experiment [2]: | |
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Animal models |
Female homozygous BALB/c Nu/Nu nude mice were injected subcutaneously (s.c.) in both flanks at 7 weeks of age with 106 parental and IKKαδ MIA PaCa-2 cells or 1334 and 1444 cells mixed at a 1:1 dilution with BD Matrigel (BD Biosciences) in a total volume of 100 µl. |
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Preparation Method |
Mice were treated with vehicle (DMSO in PBS), EIPA (7.5 mg/kg), MRT68921 (10 mg/kg) or MRT68921+EIPA for 15 days when tumors attained an average volume of 50-100 mm3. |
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Dosage form |
s.c., 7.5 mg/kg/d for 7 days |
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Applications |
One month of EIPA treatment, initiated at age 1 month, markedly reduced pancreatic weight (a tumor burden surrogate), inhibited acinar-to-ductal metaplasia (ADM) and advanced PanIN formation, and preserved the normal pancreatic parenchyma in KrasG12D;IkkαδPEC mice, while decreasing MP. |
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References: |
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| Cas No. | 1154-25-2 | SDF | |
| Synonyms | L-593,754, MH 12-43, 5-(N-ethyl-N-isopropyl)-Amiloride | ||
| 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 | ||
| Formula | C11H18ClN7O | M.Wt | 299.76 |
| Solubility | 14mg/mL in DMSO, 20mg/mL in DMF, 2mg/mL in Ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.336 mL | 16.68 mL | 33.36 mL |
| 5 mM | 667.2 μL | 3.336 mL | 6.672 mL |
| 10 mM | 333.6 μL | 1.668 mL | 3.336 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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After adding the inhibitors namely EIPA(GLPBIO)(10 μM), nystatin (10 μg mL−1), filipin III (1 μg mL−1), and CPZ (1 μg mL−1) and incubating for 30 min, the cells were washed with PBS and fresh medium was added to carry out the force tracing experiment.
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Related Biological Data
STAT3 is constitutively phosphorylated in NHE1 overexpressed gastric cancer cells.NHE1 overexpression induced the increase in the expression of pSTAT3, EIPA reverses the increase. Also, NHE1-siRNA transfection decrease the expression of pSTAT3 (Figure 5A, P<0.01).
NHE1 inhibitor EIPA (25 μM, GLPBIO,) was dissolved and stocked in DMSO and applied to the cells in the culture medium.
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Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)