NF 279A highly selective, competitive, and reversible ATP-antagonist of P2X receptor

NF 279 (CAS 202983-32-2)

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Synonym: 8,8'-[Carbonylbis(imino-4,1-phenylen ecarbonylimino-4,1-phenylenecarbonylimino)]bis-1,3 ,5-naphthalenetrisulfonic acid hexasodium salt
Application: A highly selective, competitive, and reversible ATP-antagonist of P2X receptor
CAS Number: 202983-32-2
Molecular Weight: 1401.12
Molecular Formula: C49H30N6O23S66Na
* Refer to Certificate of Analysis for lot specific data (including water content).
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NF 279 is a suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC50/KB ~ 1 μM in smooth muscle). Effectively discriminates between P2Y and P2X receptors with no effect on α1A adrenoceptors, adenosine A1 and A2B receptors, histamine H1, muscarinic M3 and neuronal nicotinic acetylcholine receptors. Displays a selectivity profile of P2X1 >P2X2 >P2X3 >P2X4 (IC50 = 19 nM, 770 nM, 1.62 μM and >300 μM, respectively) in Xenopus oocytes pre-incubated with ATP. In rat and human tissues, exhibits a potency profile of rat P2X1 > human P2X1 > > rat P2X2 > rat P2X3 ~ human P2X7 > > human P2X4. Not degraded by ecto-nucleotidases.


References

Klapperstück, M., et al. 2000. Eur. J. Pharmacol. 387, 245. Rettinger, J., et al. 2000. Neuropharmacol. 39, 2044. Lambrecht, G., et al. 1999. Prog. Brain Res. 120,107. Damer, S., et al. 1998. Eur. J. Pharmacol. 350, R5.

Physical State :
Solid
Solubility :
Soluble in DMSO (14 mg/ml), and water (35 mg/ml).
Storage :
Store at 4° C
IC50 :
P2X1: IC50 = 19 nM (Xenopus oocytes pre-incubated with ATP); P2X2: IC50 = 770 nM (Xenopus oocytes pre-incubated with ATP); P2X3: IC50 = 1.62 µM (Xenopus oocytes pre-incubated with ATP); P2X4: IC50 >300 µM (Xenopus oocytes pre-incubated with ATP)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5311315
MDL Number :
MFCD01861187
SMILES :
C1=CC(=CC=C1C(=O)NC2=C3C(=CC(=CC3=C(C=C2)S(=O)(=O)[O-])S(=O)(=O)[O-])S(= O)(=O)[O-])NC(=O)C4=CC=C(C=C4)NC(=O)NC5=CC=C(C=C5)C(=O)NC6=CC=C(C=C6)C(= O)NC7=C8C(=CC(=CC8=C(C=C7)S(=O)(=O)[O-])S(=O)(=O)[O-])S(=O)(=O)[O-].[Na+ ].[Na+].[Na+].[Na+].[Na+].[Na+]

Download SDS (MSDS)

Certificate of Analysis

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