NF449 octasodium is a highly potentP2X₁receptorantagonist, withIC₅₀s of 0.28, 0.69, and 120 nM for rP2X₁, rP2X₁₊₅, P2X₂₊₃, respectively. NF449 octasodium is a G_sα-selectiveG Proteinantagonist. 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-swhile 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].

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].

1505.09

Solid

C₄₁H₂₄N₆Na₈O₂₉S₈

627034-85-9

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)