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.

Neuroscience-Neuromodulation

[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.

Cardiovascular Disease

Membrane Transporter/Ion Channel