2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein Autophagy Immunology/Inflammation
  3. TRP Channel Prostaglandin Receptor Autophagy COX Na+/H+ Exchanger (NHE)
  4. 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.

EIPA Chemical Structure

EIPA Chemical Structure

CAS No. : 1154-25-2

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Based on 46 publication(s) in Google Scholar

Other Forms of EIPA:

EIPA Related Antibodies

Top Publications Citing Use of Products

46 Publications Citing Use of MCE EIPA

View All TRP Channel Isoform Specific Products:

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TRPC TRPM TRPV TRPA TRPML

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DP EP FP IP TXA2/TP TXB2

View All COX Isoform Specific Products:

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COX COX-1 COX-2 COX-3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.

EIPA Related Antibodies

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 : 50 mg/mL (166.80 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
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%

COA (247 KB) LCMS (407 KB)

Handling Instructions (2659 KB)
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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EIPA Related Classifications

Help & FAQs
  • 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.

Keywords:

EIPA1154-25-2L593754 MH 12-43 EthylisopropylamilorideL 593754L-593754TRP ChannelProstaglandin ReceptorAutophagyCOXNa+/H+ Exchanger (NHE)Transient receptor potential channelsCyclooxygenaseSodium/hydrogen ExchangerSodium-hydrogen ExchangerCation channelNHE3IECsIBDsIEC-18neuronzinccalciumkainiteMKN28gastric cancercolon carcinomapancreatic carcinomarenal failureddY strain miceInhibitorinhibitorinhibit

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