NF023 hexasodium

• CAT Number: M002436
• CAS Number: 104869-31-0
• Molecular Formula: C35H20N4Na6O21S6
• Molecular Weight: 1162.88
• Purity: ≥95%
• Synonyms: hexasodium;8-[[3-[[3-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]phenyl]carbamoylamino]benzoyl]amino]naphthalene-1,3,5-trisulfonate
• InChI: InChI=1S/C35H26N4O21S6.6Na/c40-33(38-25-7-9-27(63(49,50)51)23-13-21(61(43,44)45)15-29(31(23)25)65(55,56)57)17-3-1-5-19(11-17)36-35(42)37-20-6-2-4-18(12-20)34(41)39-26-8-10-28(64(52,53)54)24-14-22(62(46,47)48)16-30(32(24)26)66(58,59)60;;;;;;/h1-16H,(H,38,40)(H,39,41)(H2,36,37,42)(H,43,44,45)(H,46,47,48)(H,49,50,51)(H,52,53,54)(H,55,56,57)(H,58,59,60);;;;;;/q;6*+1/p-6
• InChIKey: FMQURVHYTBGYSQ-UHFFFAOYSA-H
• SMILES: C1=CC(=CC(=C1)NC(=O)NC2=CC=CC(=C2)C(=O)NC3=C4C(=CC(=CC4=C(C=C3)S(=O)(=O)[O-])S(=O)(=O)[O-])S(=O)(=O)[O-])C(=O)NC5=C6C(=CC(=CC6=C(C=C5)S(=O)(=O)[O-])S(=O)(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]

NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively[1][2][3][4].
NF023 is selective for recombinant Gi alpha-1 and recombinant Go alpha (EC50 value of approximately 300 nM)[2].
NF023 inhibits P2X1 receptors in a voltage-insensitive manner. NF023 (5 and 30 μM) causes a shift of the concentration-response curve to the right without affecting the maximal response to ATP (KB=1.190.2 μM)[4].
NF023 (100 µmol/kg i.v.) antagonizes vasopressor responses to α,β-mATP but not to noradrenaline In pithed rats[3].

Reference

[1]. F Soto, et al. Antagonistic Properties of the Suramin Analogue NF023 at Heterologously Expressed P2X Receptors. Neuropharmacology. 1999 Jan;38(1):141-9.
 [Content Brief]

[2]. M Freissmuth, et al. Suramin Analogues as Subtype-Selective G Protein Inhibitors. Mol Pharmacol. 1996 Apr;49(4):602-11.
 [Content Brief]

[3]. G Lambrecht, et al. Agonists and Antagonists Acting at P2X Receptors: Selectivity Profiles and Functional Implications. Naunyn Schmiedebergs Arch Pharmacol. 2000 Nov;362(4-5):340-50.
 [Content Brief]

[4]. M Silva-Ramos, et al. Activation of Prejunctional P2x2/3 Heterotrimers by ATP Enhances the Cholinergic Tone in Obstructed Human Urinary Bladders. J Pharmacol Exp Ther. 2020 Jan;372(1):63-72.
 [Content Brief]