NF 449

Modify Date: 2024-01-12 20:01:51

NF 449 Structure
NF 449 structure
Common Name NF 449
CAS Number 627034-85-9 Molecular Weight 1505.090
Density N/A Boiling Point N/A
Molecular Formula C41H24N6Na8O29S8 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of NF 449


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].

 Names

Name nf449
Synonym More Synonyms

 NF 449 Biological Activity

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].
Related Catalog
In Vitro NF449 suppressed the rate of GTP[γS] binding to rGsα-s while barely affecting binding to rGiα-1 (IC50=140 nM), inhibits stimulation of adenylyl cyclase activity in S49 cyc− membranes (deficient in endogenous Gsα) by exogenously added Gsα-s, and blocks the coupling of β-adrenergic receptors to Gs (EC50=7.9 μM)[2].
In Vivo At a dose of 10 mg/kg, NF449 inhibits the ex vivo aggregation triggered by 5 g/ml collagen in WT mouse platelets without affecting that induced by 5 μM ADP. At a higher dose (50 mg/kg), NF449 inhibits ex vivo platelet aggregation in response to not only 10 g/ml collagen but also 5 M ADP, indicating nonselective inhibition of the P2Y1 and/or P2Y12 receptor[3].
References

[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.

 Chemical & Physical Properties

Molecular Formula C41H24N6Na8O29S8
Molecular Weight 1505.090
Exact Mass 1503.753540
PSA 682.17000
LogP 8.65700

 Synonyms

1,3-Benzenedisulfonic acid, 4,4',4'',4'''-[carbonylbis[iminobenzene-5,1,3-triylbis(carbonylimino)]]tetrakis-, sodium salt (1:8)
Octasodium 4,4',4'',4'''-{carbonylbis[iminobenzene-5,1,3-triylbis(carbonylimino)]}tetra(1,3-benzenedisulfonate)
Octasodium 4-({3-[({3,5-bis[(2,4-disulfonatophenyl)carbamoyl]phenyl}carbamoyl)amino]-5-[(2,4-disulfonatophenyl)carbamoyl]benzoyl}amino)benzene-1,3-disulfonate