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NF449 (octasodium)

CAT: 0804-HY-112461A-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-112461A-01Size:1 mg
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Description
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].
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.