1. Membrane Transporter/Ion Channel Neuronal Signaling Autophagy Immunology/Inflammation GPCR/G Protein
  2. TRP Channel Autophagy COX Prostaglandin Receptor Na+/H+ Exchanger (NHE)
  3. EIPA hydrochloride

EIPA hydrochloride  (Synonyms: L593754 hydrochloride; MH 12-43 hydrochloride; Ethylisopropylamiloride hydrochloride)

Cat. No.: HY-101840A Purity: 98.31%
COA Handling Instructions

EIPA hydrochloride (L593754 hydrochloride) est un inhibiteur de canal TRPP3 avec un IC50 de 10,5 μM. EIPA hydrochloride inhibe également les échangeurs Na+/H+ (NHE) et macropinocytose.

EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na+/H+-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.

For research use only. We do not sell to patients.

EIPA hydrochloride Chemical Structure

EIPA hydrochloride Chemical Structure

CAS No. : 1345839-28-2

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Customer Review

Based on 46 publication(s) in Google Scholar

Other Forms of EIPA hydrochloride:

Top Publications Citing Use of Products

46 Publications Citing Use of MCE EIPA hydrochloride

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na+/H+-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma[1][2][3][5].

IC50 & Target[7]

COX-2

 

In Vitro

EIPA hydrochloride (100 μM, 30 min) suppresses TRPP3-mediated Ca2+ uptake in X. laevis oocytes[1].
? EIPA hydrochloride (10-100 μM) reversibly inhibits the basal Na+ current (IC50: 19.5 μM)[1].
? EIPA hydrochloride (300 μM, 6h) enhances autophagy through NHE3 (Na+/H+-exchanger 3) in IEC-18 cells[2].
? EIPA hydrochloride (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells[3].
? EIPA hydrochloride (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn2+ entry in cerebellar granule neurons[4].
? EIPA hydrochloride (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression[5].
? EIPA hydrochloride (3 μM, 6 h) inhibits the LPS-induced increase in the level of COX-2 protein[7].

MedChemExpress (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 hydrochloride (Intravenous injection, 1 mg/kg) dose-dependently attenuates the I/R (Ischemia/reperfusion)-induced renal dysfunction in ddY strain mice[6].
? EIPA hydrochloride (oral administration, 10 mg/kg) inhibits LPS-induced inflammation in air pouch-type LPS-induced inflammation model[7].

MedChemExpress (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.
Molecular Weight

336.22

Formula

C11H19Cl2N7O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NC(Cl)=C(N(CC)C(C)C)N=C1N)NC(N)=N.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 130 mg/mL (386.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9742 mL 14.8712 mL 29.7424 mL
5 mM 0.5948 mL 2.9742 mL 5.9485 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9742 mL 14.8712 mL 29.7424 mL 74.3561 mL
5 mM 0.5948 mL 2.9742 mL 5.9485 mL 14.8712 mL
10 mM 0.2974 mL 1.4871 mL 2.9742 mL 7.4356 mL
15 mM 0.1983 mL 0.9914 mL 1.9828 mL 4.9571 mL
20 mM 0.1487 mL 0.7436 mL 1.4871 mL 3.7178 mL
25 mM 0.1190 mL 0.5948 mL 1.1897 mL 2.9742 mL
30 mM 0.0991 mL 0.4957 mL 0.9914 mL 2.4785 mL
40 mM 0.0744 mL 0.3718 mL 0.7436 mL 1.8589 mL
50 mM 0.0595 mL 0.2974 mL 0.5948 mL 1.4871 mL
60 mM 0.0496 mL 0.2479 mL 0.4957 mL 1.2393 mL
80 mM 0.0372 mL 0.1859 mL 0.3718 mL 0.9295 mL
100 mM 0.0297 mL 0.1487 mL 0.2974 mL 0.7436 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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EIPA hydrochloride
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HY-101840A
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