A 740003

Pricing Availability   Qty
Cat.No. 3701 - A 740003 | C26H30N6O3 | CAS No. 861393-28-4
Description: Potent and selective P2X7 antagonist
Chemical Name: N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide
Purity: ≥98% (HPLC)
Datasheet
Citations (13)
Reviews
Literature (5)

Biological Activity

Potent and selective P2X7 receptor antagonist (IC50 values are 18 and 40 nM for rat and human receptors respectively). Displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. Reduces nociception in animal models of persistent neuropathic and inflammatory pain. Also reduces neuroblastoma tumor growth in mice.

Compound Libraries

A 740003 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 474.55
Formula C26H30N6O3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 861393-28-4
PubChem ID 11351968
InChI Key PUHSRMSFDASMAE-UHFFFAOYSA-N
Smiles CC(C)(C)C(NC(CC3=CC(OC)=C(OC)C=C3)=O)N/C(NC2=CC=CC1=NC=CC=C12)=N/C#N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 9.49 20

Preparing Stock Solutions

The following data is based on the product molecular weight 474.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 10.54 mL 52.68 mL 105.36 mL
1 mM 2.11 mL 10.54 mL 21.07 mL
2 mM 1.05 mL 5.27 mL 10.54 mL
10 mM 0.21 mL 1.05 mL 2.11 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:

References

References are publications that support the biological activity of the product.

Honore et al (2006) A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino)methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J.Pharmacol.Exp.Ther. 319 1376 PMID: 16982702

King (2007) Novel P2X7 receptor antagonists ease the pain. Br.J.Pharmacol. 151 565 PMID: 17471176

Donnelly-Roberts et al (2009) Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br.J.Pharmacol. 157 1203 PMID: 19558545

Amoroso et al (2015) The P2X7 receptor is a key modulator of the PI3K/GSK3β/VEGF signaling network: evidence in experimental neuroblastoma. Oncogene 34 5240 PMID: 25619831


If you know of a relevant reference for A 740003, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Purinergic (P2X) Receptor Antagonists

Keywords: A 740003, A 740003 supplier, A740003, potent, selective, P2X7, receptors, antagonists, purinergics, purinoceptors, P2X, Receptors, 3701, Tocris Bioscience

13 Citations for A 740003

Citations are publications that use Tocris products. Selected citations for A 740003 include:

Bergamin et al (2019) Role of the P2X7 receptor in in vitro and in vivo glioma tumor growth. Oncotarget 10 4840 PMID: 31448051

Gilbert et al (2019) ATP in the tumour microenvironment drives expression of nfP2X7, a key mediator of cancer cell survival. Oncogene 38 194 PMID: 30087439

Zumerle et al (2019) Intercellular Calcium Signaling Induced by ATP Potentiates Macrophage Phagocytosis. Cell Rep 27 1 PMID: 30943393

Englezou et al (2015) P2X7R activation drives distinct IL-1 responses in dendritic cells compared to macrophages. Cytokine 74 293 PMID: 26068648


Do you know of a great paper that uses A 740003 from Tocris? Please let us know.

Reviews for A 740003

There are currently no reviews for this product. Be the first to review A 740003 and earn rewards!

Have you used A 740003?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
Ion Channel

Ion Channel Product Listing

A collection of around 500 products for ion channel research, the listing includes research tools for the study of:

  • Ligand-gated ion channels
  • Voltage-gated ion channels
  • Other Ion Channels
Pain

Pain Research Product Guide

A collection of over 280 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
P2X and P2Y Receptors

P2X and P2Y Receptors Scientific Review

Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.

Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.