| 货号 | 13324-1mg |
| 描述 | NF449 is an analog of suramin that selectively inhibits P2X1 purinergic receptors (pIC50 = 6.3) with a potency 19-fold greater than at P2X3, P2Y1, P2Y2, or P2Y11.1,2 Through selective inhibition of the P2X1 receptor, 10 mg/kg NF449 has been used to decrease intravascular platelet aggregation in a mouse model of systemic thromboembolism.3 NF449 has also demonstrated selective antagonism of the Gsα-subunit G protein, which suppresses the association rate of GTPγS binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks G protein coupling to certain GPCRs.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kassack, M.U.,Braun, K.,Ganso, M., et al. Structure-activity relationships of analogues of NF449 confirm NF449 as the most potent and selective known P2X1 receptor antagonist. European Journal of Medicinal Chemistry 39(4), 345-357 (2004). 2.El-Ajouz, S.,Ray, D.,Allsopp, R.C., et al. Molecular basis of selective antagonism of the P2X1 receptor for ATP by NF449 and suramin: Contribution of basic amino acids in the cysteine-rich loop. British Journal of Pharmacology 165(2), 390-400 (2012). 3.Hechler, B.,Magnenat, S.,Zighetti, M.L., 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]. Journal of Pharmacology and Experimental Therapeutics 314(1), 232-243 (2005). 4.Hohenegger, M.,Waldhoer, M.,Beindl, W., et al. Gsα-selective G protein antagonists. Proceedings of the National Academy of Sciences of the United States of America 95(1), 346-351 (1998). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 1505.1 |
| 分子式 | C41H24N6O29S8 • 8Na |
| CAS号 | 627034-85-9 |
| 稳定性 | ≥ 2 years |
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