627034-85-9

627034-85-9 structure

Name: NF 449
Chemical Name: nf449
CAS Number: 627034-85-9
Molecular Formula: C₄₁H₂₄N₆Na₈O₂₉S₈
Molecular Weight: 1505.090
Catalog: Signaling Pathways Membrane Transporter/Ion Channel P2X Receptor
Create Date: 2016-06-01 05:35:39
Modify Date: 2024-01-12 20:01:51
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].

Name	nf449
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

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	Research Areas >> Cardiovascular Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor
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.

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

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