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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
HSC-4 cells 25 µM 24 hours Inhibited the uptake of HSC-4-derived exosomes by HSC-4 cells PMC8819298
Human neutrophils 75 μM 5 hours EIPA triggers NETotic cell death accompanied by an increase in intracellular ROS PMC8105669
IEC18 cells 50 µM 1 hour No significant effect on EV uptake in non-transformed cells PMC8191585
RAS3 cells 50 µM 1 hour Inhibited EV uptake via macropinocytosis in RAS3 cells PMC8191585
A549 cells 10 μM 30 min pretreatment EIPA strongly inhibited LCMV multiplication in A549 cells PMC3911747
BHK-21 cells 5-10 μM 30 min pretreatment EIPA strongly inhibited LCMV multiplication in BHK-21 cells PMC3911747
TZM-bl cells 50 μM 30 minutes Inhibition of HIV-1 infection PMC10510587
HeLa-derived cells 50 μM 30 minutes Inhibition of HIV-1 infection PMC10510587
293T cells 10 μM EIPA significantly inhibited LCMV multiplication in 293T cells PMC3911747
HTcEpi cells 20 µM 2 hours EIPA significantly reduced belantamab-specific cell killing from 34.5% to 15.5%. PMC11532697
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. PMC9761853
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. PMC10876205
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. PMC10876205
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. PMC4931471
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. PMC4931471
AsPC-1 human pancreatic cancer cells 5 μM 48 hours EIPA significantly decreased the clonogenic survival of AsPC-1 cells, indicating a radiosensitizing effect. PMC9761853
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. PMC9761853
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. PMC9306097
Rat glomerular mesangial cells (GMC) 10 µM EIPA completely prevented aldosterone-induced alkalinization by inhibiting Na+/H+ exchange. PMC8468551

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
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. PMC10876205
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. PMC9761853

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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