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A-740003

Catalog No.
A3136
P2X7 receptor antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$75.00
In stock
50mg
$70.00
In stock
100mg
$113.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

A-740003 (CAS: 861393-28-4) is a selective and competitive antagonist targeting the P2X7 receptor, a member of the ATP-gated ionotropic P2X receptor family involved in immune cell signaling, cytokine secretion, apoptosis, and cellular proliferation. The antagonist displays IC50 values of 18 nM and 40 nM against mouse and human P2X7 receptors, respectively. In human THP-1 macrophage-like cells, A-740003 inhibits pore formation assessed by Yo-Pro uptake assay (IC50 = 92 nM) and reduces interleukin-1β secretion (IC50 = 156 nM). This compound is employed in research investigating P2X7-mediated inflammatory pathways and neuropathic pain mechanisms.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt474.57
Cas No.861393-28-4
FormulaC26H30N6O3
SynonymsA 740003;A740003
Solubility≥23.73 mg/mL in DMSO; insoluble in H2O; ≥2.48 mg/mL in EtOH with gentle warming and ultrasonic
Chemical NameN-[1-[(E)-[(cyanoamino)-(quinolin-5-ylamino)methylidene]amino]-2,2-dimethylpropyl]-2-(3,4-dimethoxyphenyl)acetamide
SDFDownload SDF
Canonical SMILESCC(C)(C)C(NC(=O)CC1=CC(=C(C=C1)OC)OC)N=C(NC#N)NC2=CC=CC3=C2C=CC=N3
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description A-740003 is potent, selective and competitive antagonist of P2X7 receptor with IC50 values of 18 nM and 40 nM for rat and human receptors, respectively.
Targets P2X7 receptor          
IC50 18 nM (rat) 40 nM (human)          

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