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Chemical Structure| 1154-25-2 Chemical Structure| 1154-25-2

Structure of EIPA
CAS No.: 1154-25-2

Chemical Structure| 1154-25-2

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EIPA (L593754) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.

Synonyms: L593754; MH 12-43; 5-(N-ethyl-N-isopropyl)-Amiloride

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Product Details of EIPA

CAS No. :1154-25-2
Formula : C11H18ClN7O
M.W : 299.76
SMILES Code : O=C(C1=NC(Cl)=C(N(CC)C(C)C)N=C1N)NC(N)=N
Synonyms :
L593754; MH 12-43; 5-(N-ethyl-N-isopropyl)-Amiloride
MDL No. :MFCD00151710

Safety of EIPA

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HeLa-derived cells 50 µM 30 minutes Inhibition of HIV-1 infection ACS Nano. 2023 Sep 12;17(17):17436-17450.
293T cells 10 µM EIPA significantly inhibited LCMV multiplication in 293T cells J Virol. 2014 Jan;88(1):643-54.
TZM-bl cells 50 µM 30 minutes Inhibition of HIV-1 infection ACS Nano. 2023 Sep 12;17(17):17436-17450.
RAS3 cells 50 µM 1 hour Inhibited EV uptake via macropinocytosis in RAS3 cells J Extracell Vesicles. 2021 Jun;10(8):e12091.
HSC-4 cells 25 µM 24 hours Inhibited the uptake of HSC-4-derived exosomes by HSC-4 cells Cancer Sci. 2022 Feb;113(2):609-621.
IEC18 cells 50 µM 1 hour No significant effect on EV uptake in non-transformed cells J Extracell Vesicles. 2021 Jun;10(8):e12091.
HTcEpi cells 20 µM 2 hours EIPA significantly reduced belantamab-specific cell killing from 34.5% to 15.5%. Haematologica. 2024 Nov 1;109(11):3670-3680.
MDA-MB-231RR radioresistant cells 20 µM or 50 µM 24 hours EIPA treatment reversed the transcriptomic changes in radioresistant cells, downregulating NF-κB, senescence, and extracellular matrix-related genes. Neoplasia. 2023 Jan;35:100862.
A549 cells 10 µM 30 min pretreatment EIPA strongly inhibited LCMV multiplication in A549 cells J Virol. 2014 Jan;88(1):643-54.
BHK-21 cells 5-10 µM 30 min pretreatment EIPA strongly inhibited LCMV multiplication in BHK-21 cells J Virol. 2014 Jan;88(1):643-54.
MHCC97L cells 35 or 75 µM 30 minutes To evaluate the effect of EIPA on macropinocytosis and sEV uptake. The results showed that EIPA significantly reduced the uptake of TMR-dextran and PKH67-sEVs. Cancer Commun (Lond). 2024 Feb;44(2):251-272.
MHCCLM3 cells 35 or 75 µM 30 minutes To evaluate the effect of EIPA on macropinocytosis and sEV uptake. The results showed that EIPA significantly reduced the uptake of TMR-dextran and PKH67-sEVs. Cancer Commun (Lond). 2024 Feb;44(2):251-272.
Mouse skin fibroblasts (MSF) 10 µM 30 seconds To detect the inhibitory effect of EIPA on NHE, results showed a significant response to EIPA in NHE3-reconstituted MSF cells, while NHE-deficient MSF cells showed no response. Biosensors (Basel). 2016 Mar 30;6(2):11.
Chinese hamster ovary (CHO) cells 10 µM 30 seconds To detect the inhibitory effect of EIPA on NHE, results showed a significant response to EIPA inhibition in CHO cells. Biosensors (Basel). 2016 Mar 30;6(2):11.
AsPC-1 human pancreatic cancer cells 5 µM 48 hours EIPA significantly decreased the clonogenic survival of AsPC-1 cells, indicating a radiosensitizing effect. Neoplasia. 2023 Jan;35:100862.
MDA-MB-231 human breast cancer cells 5 µM 48 hours EIPA significantly decreased the plating efficiency of MDA-MB-231 cells from 52% to 35%, indicating a radiosensitizing effect. Neoplasia. 2023 Jan;35:100862.
U373-MG cells 25 µM 48 or 72 hours EIPA significantly increased the autophagic response induced by trehalose, and the effect of combined molecules appeared to be synergistic at 48 and 72 hours of treatment. Cancer Cell Int. 2022 Jul 21;22(1):232.
Human neutrophils 75 µM 5 hours EIPA triggers NETotic cell death accompanied by an increase in intracellular ROS Redox Biol. 2021 Jul;43:101983.
Rat glomerular mesangial cells (GMC) 10 µM EIPA completely prevented aldosterone-induced alkalinization by inhibiting Na+/H+ exchange. Biomedicines. 2021 Aug 30;9(9):1117.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice MDA-MB-231 xenograft tumor model Intraperitoneal injection 12 mg/kg Three times a week for the first two weeks, then twice a week for the next two weeks, lasting four weeks Combination therapy of EIPA and radiation significantly inhibited the growth of MDA-MB-231 xenograft tumors, increased apoptotic cells in tumor tissues, and reduced the expression of NHE1 and phospho-NF-κB p65. Neoplasia. 2023 Jan;35:100862.
BALB/cAnN-nu mice Subcutaneous xenograft model Subcutaneous injection 5 mg/kg Single injection To evaluate the effect of EIPA on sEV-induced tumor growth. The results showed that EIPA significantly inhibited sEV-induced tumor growth. Cancer Commun (Lond). 2024 Feb;44(2):251-272.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.34mL

0.67mL

0.33mL

16.68mL

3.34mL

1.67mL

33.36mL

6.67mL

3.34mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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