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 G_sα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to G_sα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to G_s^[1][2].

NF449 suppressed the rate of GTP[γS] binding to rG_sα-s while barely affecting binding to rG_iα-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 G_s (EC₅₀=7.9 μM)^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1505.09

Solid

C₄₁H₂₄N₆Na₈O₂₉S₈

627034-85-9

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

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

• [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.  [Content Brief]

  [2]. Hohenegger M, et al. Gsalpha-selective G protein antagonists. Proc Natl Acad Sci U S A. 1998;95(1):346-351.  [Content Brief]

  [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-be  [Content Brief]