[CAS NO. 1154-25-2] EIPA
PRODUCTS SPECIFICATIONS [1154-25-2]
DESCRIPTION [1154-25-2]
Overview
| MDL | MFCD00151710 |
|---|---|
| Molecular Weight | 299.76 |
| Molecular Formula | C11H18ClN7O |
| SMILES | O=C(C1=NC(Cl)=C(N(CC)C(C)C)N=C1N)NC(N)=N |
32 Publications Citing Use of MCE
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- [2]Adv Funct Mater. 2021 Apr 1.
- [3]ACS Nano. 2020 Nov 24;14(11):14698-14714.
- [4]Sci Adv. 2020 Aug 12;6(33):eaaz1774.
- [5]J Exp Med. 2023 Mar 6;220(3):e20221316.
- [6]Biomaterials. 13 January 2022, 121373.
- [7]Autophagy. 2022 Aug 1;1-19.
- [8]Genes Dev. 2021 Oct 1;35(19-20):1327-1332.
- [9]J Hazard Mater. 2021 Sep 5;417:126092.
- [10]ACS Appl Mater Interfaces. 2020 Oct 14;12(41):45763-45771.
- [11]Theranostics. 2022 Jan 1;12(3):1061-1073.
- [12]Theranostics. 2022; 12(3):1061-1073.
- [13]J Control Release. 2022 Oct 7;351:703-712.
- [14]Comput Struct Biotec. 2021;19:1933-1943.
- [15]Anal Chem. 2020 Jan 21;92(2):2103-2111.
- [16]J Nanobiotechnology. 2022 Jul 20;20(1):340.
- [17]J Nanobiotechnology. 2022 Jun 10;20(1):268.
- [18]Sci China Mater. 63, 620-628 (2020).
- [19]Biomacromolecules. 2021 Aug 12.
- [20]Emerg Microbes Infect. 2022 Dec;11(1):1135-1144.
- [21]Nanotoxicology. 2023 Jan 26;1-18.
- [22]Drug Deliv. 2021 Dec;28(1):800-813.
- [23]Bioorg Chem. 2022 Feb 12;121:105651.
- [24]Sci China Life Sci. 2021 May 27;1-21.
- [25]J Virol. 2021 Sep 29;JVI0134521.
- [26]Pharmaceutics. 2020 Feb 17;12(2):167.
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- [28]J Biol Chem. 19 September 2022, 102511.
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Summary
EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC 50 of 10.5 μM. EIPA also enhances autophagy by inhibiting Na + /H + -exchanger 3 ( NHE3 ). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer , colon carcinoma, pancreatic carcinoma [1] [2] [3] [5] .
IC50 & Target
|
COX-2 |
In Vitro
EIPA (100 μM, 30 min) suppresses TRPP3-mediated Ca
2+
uptake in
X. laevis oocytes
[1]
.
EIPA hydrochloride (10-100 μM) reversibly inhibits the basal Na
+
current (IC
50
: 19.5 μM)
[1]
.
EIPA (300 μM, 6h) enhances autophagy through NHE3 (Na
+
/H
+
-exchanger 3) in IEC-18 cells
[2]
.
EIPA (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells
[3]
.
EIPA (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn
2+
entry in cerebellar granule neurons
[4]
.
EIPA (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression
[5]
.
EIPA (3 μM, 6 h) inhibits the LPS-induced increase in the level of COX-2 protein
[7]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [5]
| Cell Line: | MKN28 cells |
| Concentration: | 5, 10, 25, 50, and 100 μM |
| Incubation Time: | 48 h |
| Result: | Inhibited cell proliferation in a dose- and time-dependent manner. |
Western Blot Analysis [2]
| Cell Line: | IEC-18 cells |
| Concentration: | 300 μM |
| Incubation Time: | 6 h |
| Result: |
Increased total LC3-II protein levels and P62 flux.
Increased ATG5, 7, 12 and P62 expression. |
In Vivo
EIPA (Intravenous injection, 1 mg/kg) dose-dependently attenuates the I/R (Ischemia/reperfusion)-induced renal dysfunction in ddY strain mice
[6]
.
EIPA (oral administration, 10 mg/kg) inhibits LPS-induced inflammation in air pouch-type LPS-induced inflammation model
[7]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male ddY strain mice [6] |
| Dosage: | 1 mg/kg |
| Administration: | Intravenous injection |
| Result: | Attenuated histologic renal damage, and imprved the I/R-induced increases in renal ET-1 contents. |
| Animal Model: | Air pouch-type LPS-induced inflammation model [7] |
| Dosage: | 10 mg/kg |
| Administration: | Oral administration |
| Result: |
Inhibited the LPS-induced infiltration of leukocytes into the pouch.
Inhibited the amount of PGE2 in the pouch fluid. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 166.80 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (ultrasonic) (insoluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3360 mL | 16.6800 mL | 33.3600 mL |
| 5 mM | 0.6672 mL | 3.3360 mL | 6.6720 mL |
| 10 mM | 0.3336 mL | 1.6680 mL | 3.3360 mL |
-
1.
References
- [1] Dai XQ, et al. Inhibition of TRPP3 channel by MK-870 and analogs. Mol Pharmacol. 2007 Dec;72(6):1576-85.
- [2] Shi H, et al. Na+/H+ Exchanger Regulates Amino Acid-Mediated Autophagy in Intestinal Epithelial Cells. Cell Physiol Biochem. 2017;42(6):2418-2429.
- [3] Zhu BY, et al. A new HDAC inhibitor cinnamoylphenazine shows antitumor activity in association with intensive macropinocytosis.
- [4] E V Stelmashook, et al. Acidosis and 5-(N-ethyl-N-isopropyl)amiloride (EIPA) Attenuate Zinc/Kainate Toxicity in Cultured Cerebellar Granule Neurons. Biochemistry (Mosc). 2015 Aug;80(8):1065-72.
- [5] Shigekuni Hosogi, et al. 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(5):1241-53.
- [6] Junji Yamashita, et al. Role of Na+/H+ exchanger in the pathogenesis of ischemic acute renal failure in mice. J Cardiovasc Pharmacol. 2007 Mar;49(3):154-60.
- [7] Fumitaka Kamachi, et al. Inhibition of lipopolysaccharide-induced prostaglandin E2 production and inflammation by the Na+/H+ exchanger inhibitors. J Pharmacol Exp Ther. 2007 Apr;321(1):345-52.
Synonyms
