A-740003
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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.


Chemical Structure

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A-740003
CAS# 861393-28-4

Theoretical Analysis

MedKoo Cat#: 526702
Name: A-740003
CAS#: 861393-28-4
Chemical Formula: C26H30N6O3
Exact Mass: 474.24
Molecular Weight: 474.565
Elemental Analysis: C, 65.80; H, 6.37; N, 17.71; O, 10.11

Price and Availability

Size Price Availability Quantity
10mg USD 550 2 Weeks
50mg USD 1650 2 Weeks
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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

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).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 474.57 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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: 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. doi: 10.1124/jpet.106.111559. Epub 2006 Sep 18. PMID: 16982702.


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15: Englezou PC, Rothwell SW, Ainscough JS, Brough D, Landsiedel R, Verkhratsky A, Kimber I, Dearman RJ. P2X7R activation drives distinct IL-1 responses in dendritic cells compared to macrophages. Cytokine. 2015 Aug;74(2):293-304. doi: 10.1016/j.cyto.2015.05.013. Epub 2015 Jun 9. PMID: 26068648; PMCID: PMC4504032.


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18: Grol MW, Brooks PJ, Pereverzev A, Dixon SJ. P2X7 nucleotide receptor signaling potentiates the Wnt/β-catenin pathway in cells of the osteoblast lineage. Purinergic Signal. 2016 Sep;12(3):509-20. doi: 10.1007/s11302-016-9517-4. Epub 2016 May 21. PMID: 27206526; PMCID: PMC5023632.


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20: Gulinelli S, Salaro E, Vuerich M, Bozzato D, Pizzirani C, Bolognesi G, Idzko M, Di Virgilio F, Ferrari D. IL-18 associates to microvesicles shed from human macrophages by a LPS/TLR-4 independent mechanism in response to P2X receptor stimulation. Eur J Immunol. 2012 Dec;42(12):3334-45. doi: 10.1002/eji.201142268. Epub 2012 Oct 26. PMID: 22996386.