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].

Product Specifications

CAS Number

[627034-85-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

P2X Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/nf449-octasodium.html

Purity

99.0

Solubility

H2O : 10 mg/mL (ultrasonic; warming) |DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C41H24N6Na8O29S8

Molecular Weight

1505.09

Precautions

H302, H315, H319, H335

References & Citations

[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.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C (Powder, stored under nitrogen)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

P2X1 Receptor

Citation 01

Cell Host Microbe. 2025 Sep 30:S1931-3128 (25) 00375-0.|Proc Natl Acad Sci U S A. 2024 Oct 29;121 (44) :e2318767121.|Vet Parasitol. 2022 Dec:312:109841.|EMBO J. 2025 Sep 1.