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 抑制 GTP[γS] 与 rG_sα-s 的结合速率，而几乎不影响与 rG_iα-1 的结合 (IC₅₀=140 nM)，通过外源添加的 Gsα-s 抑制 S49 环化膜 (缺乏内源性 Gsα) 中腺苷酸环化酶活性的刺激，并阻断 β-肾上腺素能受体与 G_s 的偶联 (EC₅₀=7.9 μM)^[2]。

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

在 10 mg/kg 的剂量下，NF449 抑制由 5 g/mL 胶原蛋白在 WT 小鼠血小板中触发的离体聚集，而不影响由 5 μM ADP 诱导的聚集。在较高剂量 (50 mg/kg) 下，NF449 抑制离体血小板聚集，不仅响应 10 g/mL 胶原蛋白，还响应 5 M ADP，表明非选择性抑制 P2Y1 和/或 P2Y12 受体^[3]。

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

1329.24

C₄₁H₃₂N₆O₂₉S₈

389142-38-5

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]