A 740003 CAS: 861393-28-4
MF: C26H30N6O3
MW: 474.56
A potent, selective and competitive P2X7 receptor antagonist.

A 740003 (CAS 861393-28-4)

A 740003 | CAS 861393-28-4 is rated 5.0 out of 5 by 1.
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Synonym: N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]- 2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide
Application: A 740003 is a potent, selective and competitive P2X7 receptor antagonist
CAS Number: 861393-28-4
Purity: ≥98%
Molecular Weight: 474.56
Molecular Formula: C26H30N6O3
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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A 740003 is a competitive antagonist of P2X7 receptors that has been shown to potently block proinflammatory cytokine interleukin-1β (IL-1β) release. Experiments have reported that a slight activation of P2X7 receptors causes a rapid increase in the opening of non-selective cation channels. P2X7 receptors are ATP-sensitive and localized on cells of immunological origin.


References

1. Honore, P., et al. 2006. J. Pharmacol. Exp. Ther. 319: 1376-1385. PMID: 16982702
2. King, B.F. 2007. Br. J. Pharmacol. 151: 565-567. PMID: 17471176
3. Donnelly-Roberts, D.L., et al. 2009. Br. J. Pharmacol. 157: 1203-1214. PMID: 19558545

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (5 mM).
Storage :
Store at 4° C
Melting Point :
128-129° C
Boiling Point :
679.94° C (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D ~1.60 (Predicted)
IC50 :
P2X7 receptor: IC50 = 18 nM (rat); P2X7 receptor: IC50 = 40 nM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
Transport :
UN 2811, Class 6.1, Packing group III
PubChem CID :
23232014
MDL Number :
MFCD09970333
SMILES :
CC(C)(C)C(NC(=O)CC1=CC(=C(C=C1)OC)OC)/N=C(/NC#N)\\NC2=CC=CC3=C2C=CC=N3

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Certificate of Analysis

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A 740003  Product Citations

See how others have used A 740003. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 30138927  Piippo, N. et al. 2018. Cell. Physiol. Biochem. 49: 359-367.

PMID: # 21505260  Kim, JE. et al. 2011. J. Clin. Invest. 121: 2037-47.

PMID: # 27122036  J. Neurosci. 36: 4785-801.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from Gicquel T; et al Gicquel T; et al. (PubMed ID: 26116704) determined A 740003, a P2X7 purinergic receptor antagonist, significantly blocked IL-1 production and pro-IL-1 cleavage. -SCBT Publication Review
Date published: 2015-05-29
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