A-740003
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526702

CAS#: 861393-28-4

Description: A-740003 is a potent and selective P2X7 receptor antagonist. A-740003 has (IC(50) values = 40 nM for human and 18 nM for rat) as measured by agonist-stimulated changes in intracellular calcium concentrations. A-740003 showed weak or no activity (IC(50) > 10 muM) at other P2 receptors and an array of other neurotransmitter and peptide receptors, ion channels, reuptake sites, and enzymes. A-740003 potently blocked agonist-evoked IL-1beta release (IC(50) = 156 nM) and pore formation (IC(50) = 92 nM) in differentiated human THP-1 cells. A-740003 in vivo produces significant antinociception in animal models of neuropathic and inflammatory pain.


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A-740003, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 526702
Name: A-740003
CAS#: 861393-28-4
Chemical Formula: C26H30N6O3
Exact Mass: 474.2379
Molecular Weight: 474.565
Elemental Analysis: C, 65.80; H, 6.37; N, 17.71; O, 10.11


Synonym: A-740003; A 740003; A740003.

IUPAC/Chemical Name: N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide

InChi Key: PUHSRMSFDASMAE-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H30N6O3/c1-26(2,3)24(31-23(33)15-17-11-12-21(34-4)22(14-17)35-5)32-25(29-16-27)30-20-10-6-9-19-18(20)8-7-13-28-19/h6-14,24H,15H2,1-5H3,(H,31,33)(H2,29,30,32)

SMILES Code: O=C(NC(/N=C(NC#N)\NC1=C2C=CC=NC2=CC=C1)C(C)(C)C)CC3=CC=C(OC)C(OC)=C3


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Janssen B, Vugts DJ, Funke U, Spaans A, Schuit RC, Kooijman E, Rongen M, Perk
LR, Lammertsma AA, Windhorst AD. Synthesis and initial preclinical evaluation of
the P2X7 receptor antagonist [¹¹C]A-740003 as a novel tracer of
neuroinflammation. J Labelled Comp Radiopharm. 2014 Jun 30;57(8):509-16. doi:
10.1002/jlcr.3206. Epub 2014 Jul 3. PubMed PMID: 24995673.

2: Honore P, Donnelly-Roberts D, Namovic MT, Hsieh G, Zhu CZ, Mikusa JP,
Hernandez G, Zhong C, Gauvin DM, Chandran P, Harris R, Medrano AP, Carroll W,
Marsh K, Sullivan JP, Faltynek CR, Jarvis MF. 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. 2006 Dec;319(3):1376-85. Epub 2006 Sep 18. PubMed
PMID: 16982702.