| Bioactivity | 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 Gsα-selective G Protein antagonist. NF449 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]. |
| Invitro | NF449 抑制 GTP[γS] 与 rGsα-s 的结合速率，而几乎不影响与 rGiα-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 Gs 的偶联 (EC50=7.9 μM)[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> NF449 相关抗体: |
| In Vivo | 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. |
| CAS | 389142-38-5 |
| Formula | C41H32N6O29S8 |
| Molar Mass | 1329.24 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
NF449
CAS: 389142-38-5 F: C41H32N6O29S8 W: 1329.24
NF449 is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, resp
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