Home Neuronal Signaling P2 Receptor antagonist - Interleukins inhibitor A-740003 For research use only.

A-740003

A-740003 is a potent, selective and competitive antagonist of P2X7 receptor with IC50 of 18 nM and 40 nM for rat and human P2X7 receptors, respectively. A-740003 potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells.

A-740003 Chemical Structure

A-740003 Chemical Structure

CAS No. 861393-28-4

Purity & Quality Control

A-740003 Related Products

Signaling Pathway

P2 Receptor Signaling Pathways

P2 Receptor Signaling Pathway

Biological Activity

Description A-740003 is a potent, selective and competitive antagonist of P2X7 receptor with IC50 of 18 nM and 40 nM for rat and human P2X7 receptors, respectively. A-740003 potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells.
Targets
rat P2X7 receptor [1]
(Cell-free assay)		 human P2X7 receptor [1]
(Cell-free assay)		 IL-1β pore formation [1]
(Cell-based assay)		 IL-1β release [1]
(Cell-based assay)
18 nM 40 nM 92 nM 156 nM

Chemical Information & Solubility

Molecular Weight 474.55 Formula

C26H30N6O3
CAS No. 861393-28-4 SDF --
Smiles CC(C)(C)C(NC(=O)CC1=CC(=C(C=C1)OC)OC)N=C(NC#N)NC2=CC=CC3=C2C=CC=N3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 95 mg/mL ( (200.18 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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