NF449 

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 G_sα-selective G Protein antagonist. NF449 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].

MedChemExpress (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].

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

1329.24

C₄₁H₃₂N₆O₂₉S₈

389142-38-5

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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-benzene-1,3-disulfonic acid octasodium salt]. J Pharmacol Exp Ther. 2005;314(1):232-243.  [Content Brief]