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EIPA (L593754) Macropinocytosis Inhibitor

Name: EIPA (L593754)
Brand: Selleck Chemicals
SKU: S9849
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S9849

EIPA (L593754; MH 12-43) acts as an inhibitor of macropinocytosis and sodium-hydrogen exchangers(NHE) (IC50=0.033μg/mL). EIPA blocks the activity of Na(+)/H(+) exchanger, which are plasma membrane proteins implicated in all forms of macropinocytosis.

Chemical Structure

Molecular Weight: 299.76

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Quality Control

Batch: Purity: 99.77%

99.77

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor ATPase GluR
Other TRP Channel Inhibitors	SKF96365 AMG-517 HC-030031 2-APB (2-Aminoethyl Diphenylborinate) GSK2193874 Capsazepine GSK1016790A SB705498 Caffeic Acid HC-067047

Solubility

In vitro
Batch:

DMSO : 60 mg/mL (200.16 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 30 mg/mL

Water : 2 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.500mg/ml (18.35mM)	Taking the 1 mL working solution as an example, add 50 μL of 110 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.500mg/ml (18.35mM)	Taking the 1 mL working solution as an example, add 50 μL of 110 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (6.67mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	299.76	Formula	C₁₁H₁₈ClN₇O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1154-25-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	L593754; MH 12-43			Smiles	CCN(C(C)C)C1=C(Cl)N=C(C(=N1)N)C(=O)NC(N)=N

Mechanism of Action

Targets/IC₅₀/Ki	NHE (in the Sodium-hydrogen exchanger activity assay) 0.033 μg/mL
In vitro	This compound rapidly and reversibly block Ca²⁺-activated TRPP3 channel activation, with IC₅₀s of 10.5 μM.
In vivo	EIPA downregulates endothelial cell activation of NF-kappaB and VCAM-1 expression and attenuates the early inflammatory stages of atherogenesis and stent intimal formation.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24184990/ [2] https://pubmed.ncbi.nlm.nih.gov/17804601/ [3] https://pubmed.ncbi.nlm.nih.gov/15505102/

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Handling Instructions

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