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NF449

CAT: 0804-HY-112461Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-112461Size:1 Each
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Description
NF449 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 is a Gsα-selective G Protein antagonist. NF449 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].
CAS Number
389142-38-5
UNSPSC
12352005
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.html
Smiles
O=C(NC1=CC(C(NC2=CC=C(S(=O)(O)=O)C=C2S(=O)(O)=O)=O)=CC(C(NC3=CC=C(S(=O)(O)=O)C=C3S(=O)(O)=O)=O)=C1)NC4=CC(C(NC5=CC=C(S(=O)(O)=O)C=C5S(=O)(O)=O)=O)=CC(C(NC6=CC=C(S(=O)(O)=O)C=C6S(=O)(O)=O)=O)=C4
Molecular Formula
C41H32N6O29S8
Molecular Weight
1329.24
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]Hohenegger M, et al. Gsalpha-selective G protein antagonists. Proc Natl Acad Sci U S A. 1998;95 (1) :346-351.|[3]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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
P2X1 Receptor
Citation 01
EMBO J. 2025 Sep 1.|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.

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