A-740003 - CAS 861393-28-4
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
A-740003
Catalog Number:
861393-28-4
Synonyms:
N-[1-[[(Cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide;N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide
CAS Number:
861393-28-4
Description:
A-740003 is potent, selective and competitive P2X7 receptor antagonist. Its IC50 values are 18 and 40 nM for rat and human receptors respectively measured by agonist-stimulated changes in intracellular calcium concentrations. It displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. It reduces nociception in animal models of persistent neuropathic and inflammatory pain. It 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. It potently blocked agonist-evoked IL-1beta release (IC(50) = 156 nM) and pore formation (IC(50) = 92 nM) in differentiated human THP-1 cells. It produces significant antinociception in animal models of neuropathic and inflammatory pain in vivo.
Molecular Weight:
474.55
Molecular Formula:
C26H30N6O3
Quantity:
Grams-Kilos
Quality Standard:
In-house standard
COA:
Inquire
MSDS:
Inquire
Canonical SMILES:
CC(C)(C)C(NC(=O)CC1=CC(=C(C=C1)OC)OC)N=C(NC#N)NC2=CC=CC3=C2C=CC=N3
InChI:
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)
InChIKey:
PUHSRMSFDASMAE-UHFFFAOYSA-N
Targets:
P2X Receptor
Chemical Structure
CAS 861393-28-4 A-740003

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