GW274150 phosphate 是一种有效的，选择性的，口服活性的 NADPH 依赖型人一氧化氮合成酶 (iNOS) (Kd=40 nM) 和大鼠 iNOS 抑制剂，对人和大鼠 eNOS 和 nNOS 均显示较低效力。GW274150 phosphate 在急性肺损伤炎症模型中发挥保护作用。
GW274150 phosphate is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM), displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 phosphate exerts a protective role in an acute model of lung injury inflammation[1][2].
[1]. Alderton WK, et al. GW274150 and GW273629 are potent and highly selective inhibitors of inducible nitric oxide synthase in vitro and in vivo.Br J Pharmacol. 2005 Jun;145(3):301-12. [2]. Dugo L, et al. Effects of GW274150, a novel and selective inhibitor of iNOS activity, in acute lung inflammation. Br J Pharmacol. 2004 Mar;141(6):979-87. Epub 2004 Feb [3]. Broom L, et al. Neuroprotection by the selective iNOS inhibitor GW274150 in a model of Parkinson disease.Free Radic Biol Med. 2011 Mar 1;50(5):633-40.
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