NF449 (octasodium)

NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs[1][2].

O=C(NC1=CC(C(NC2=CC=C(S(=O)(O[Na])=O)C=C2S(=O)(O[Na])=O)=O)=CC(C(NC3=CC=C(S(=O)(O[Na])=O)C=C3S(=O)(O[Na])=O)=O)=C1)NC4=CC(C(NC5=CC=C(S(=O)(O[Na])=O)C=C5S(=O)(O[Na])=O)=O)=CC(C(NC6=CC=C(S(=O)(O[Na])=O)C=C6S(=O)(O[Na])=O)=O)=C4

[1]Rettinger J, et al. Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonist. Neuropharmacology. 2005;48(3):461-468.|[2]Hechler B, et al. Inhibition of platelet functions and thrombosis through selective or nonselective inhibition of the platelet P2 receptors with increasing doses of NF449 [4,4',4'',4'''-(carbonylbis(imino-5,1,3-benzenetriylbis-(carbonylimino)))tetrakis-benzene-1,3-disulfonic acid octasodium salt]. J Pharmacol Exp Ther. 2005;314(1):232-243.|[3]Hohenegger M, et al. Gsalpha-selective G protein antagonists. Proc Natl Acad Sci U S A. 1998;95(1):346-351.