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  3. EIPA

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

Cat. No.: HY-101840 Purity: 99.73%
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EIPA (L593754) est un inhibiteur de canal TRPP3 avec un IC50 de 10,5 μM. EIPA inhibe également les échangeurs Na+/H+ (NHE) et macropinocytose.

EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC50 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.

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

CAS No. : 1154-25-2

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Customer Review

Based on 98 publication(s) in Google Scholar

Other Forms of EIPA:

Top Publications Citing Use of Products

98 Publications Citing Use of MCE EIPA

Gel Electrophoresis
RT-PCR
Flow Cytometry
Cell Imaging/Staining
WB

    EIPA purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2025 Jul 15:S1535-6108(25)00271-5.  [Abstract]

    Murine CAFs were cultured in 4 mM or 0.2 mM Q with DMSO or 25 μM EIPA hydrochloride for 4 h. The protein levels of sestrin2 (SESN2) were analyzed by western blot.

    EIPA purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2025 Jul 15:S1535-6108(25)00271-5.  [Abstract]

    Murine CAFs were cultured in 4 mM or 0.2 mM Q with DMSO or 25 μM EIPA for 32 h.

    EIPA purchased from MedChemExpress. Usage Cited in: Adv Mater. 2025 Jan 10:e2415030.  [Abstract]

    EIPA (50 μM, 7 h) decreased the internalization efficiency of F/G/H-GNC in 4T1 cells by approximately 17%.

    EIPA purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Oct 9.  [Abstract]

    EIPA (30 μM, 24 h) could not completely block the signal enhancement of FITC-EV mediated by P-3 Fax-Neu5Ac in RT-112 and KU-19-19 cells.

    EIPA purchased from MedChemExpress. Usage Cited in: J Cell Biol. 2025 May 5;224(5):e202405060.  [Abstract]

    Agarose gel of Xbp1 cDNA amplicons in AML12 treated with Ctrl/CM ± endocytosis inhibitors (amiloride, nocodazole, nystatin, EIPA hydrochloride (40 μM)).

    EIPA purchased from MedChemExpress. Usage Cited in: Nat Nanotechnol. 2025 Feb;20(2):296-302.  [Abstract]

    EIPA (5 μg/mL, 24 h) could not reverse 500 nM NTZ-NPs induced EGFR protein degradation in MDA-MB-231 cells.

    EIPA purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):2018-2035.e8.  [Abstract]

    Bone marrow cells cultured in medium containing 10 ng/mL GM-CSF for 3 days were treated with 2 μg PKH67-labeled sEVs with or without Amiloride (10 μM), Chlorpromazine (10 μM), or EIPA (5 μM) for 1 h. The median fluorescence intensity (MFI) of PKH67 was assessed by flow cytometry.

    EIPA purchased from MedChemExpress. Usage Cited in: Emerg Microbes Infect. 2022 Dec;11(1):1135-1144.  [Abstract]

    The blocking effect of EIPA hydrochloride (30 μM) on dextran, CPZ (25 μM) on transferrin, and MCD (3 mM) or filipin III (1 μg/ml) on CTB was observed in Vero E6 cells. Hoechst was used to stain the nuclei.

    EIPA purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2021 Apr 1.

    EIPA (100 μM, 5 h) inhibited the intracellular uptake of antigenic peptides GT83-Mn2+/OVA257-280-FITC NPs in DC2.4 cells.

    EIPA purchased from MedChemExpress. Usage Cited in: Mol Pharm. 2021 Oct 4;18(10):3750-3762.  [Abstract]

    The cellular fluorescence profiles showed 5-TAMRA-RRL signals were sharply inhibited by Pitstop 2, EIPA hydrochloride (100 μM) and VER-155008 (20 μM).

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    • Biological Activity

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    Description

    EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC50 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][4][5][6][7].

    IC50 & Target[7]

    COX-2

     

    In Vitro

    EIPA (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 (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 Zn2+ 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].

    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 (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].

    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

    299.76

    Formula

    C11H18ClN7O

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (333.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    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
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (8.34 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (8.34 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
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    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.73%

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3360 mL 16.6800 mL 33.3600 mL 83.4001 mL
    5 mM 0.6672 mL 3.3360 mL 6.6720 mL 16.6800 mL
    10 mM 0.3336 mL 1.6680 mL 3.3360 mL 8.3400 mL
    15 mM 0.2224 mL 1.1120 mL 2.2240 mL 5.5600 mL
    20 mM 0.1668 mL 0.8340 mL 1.6680 mL 4.1700 mL
    25 mM 0.1334 mL 0.6672 mL 1.3344 mL 3.3360 mL
    30 mM 0.1112 mL 0.5560 mL 1.1120 mL 2.7800 mL
    40 mM 0.0834 mL 0.4170 mL 0.8340 mL 2.0850 mL
    50 mM 0.0667 mL 0.3336 mL 0.6672 mL 1.6680 mL
    60 mM 0.0556 mL 0.2780 mL 0.5560 mL 1.3900 mL
    80 mM 0.0417 mL 0.2085 mL 0.4170 mL 1.0425 mL
    100 mM 0.0334 mL 0.1668 mL 0.3336 mL 0.8340 mL
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      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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