GW274150 phosphate 是一种有效的，选择性的，口服活性的 NADPH 依赖型人诱导型一氧化氮合成酶 (iNOS) (K_d=40 nM) 和大鼠 (iNOS) 抑制剂。GW274150 phosphate 对人和大鼠内皮一氧化氮合酶 (eNOS) 和神经元一氧化氮合酶 (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) (IC 50 =2.19 μM; K d =40 nM) and rat iNOS (ED 50 =1.15 μM). GW274150 phosphate 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.

Solid

Kd: 40 nM (iNOS)
IC50: 2.19 μM (human iNOS); 544 μM (human eNOS); 177 μM (human nNOS)
ED50: 1.15 μM (rat iNOS); 252 μM (rat nNOS)

GW274150 phosphate inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC50 values of 0.2±0.04 μM.
GW274150 is >260-fold and 219-fold selective for iNOS against eNOS and nNOS in rat tissues, respectively. And it displays >100-fold and >80-fold for human iNOS against human eNOS and nNOS, respectively.
has not independently confirmed the accuracy of these methods. They are for reference only.

GW274150 phosphate is a long-acting (5 h half‐life in rats) iNOS inhibitor and is able to inhibit LPS‐mediated increase in plasma NO2, NO3 levels 14 h after single intraperitoneal dose (ED 50 =3 mg/kg).
GW274150 phosphate (intraperitoneal injection; 2.5, 5, and 10 mg/kg; before carrageenan injection) reduces the degree of lung injury induced by carrageenan in a dose-related fashion. Oedema formation and PMNs infiltration in the pleural cavity are also significantly attenuated in a dose‐related manner in rats.
GW274150 phosphate (oral adminstration; 30 mg/kg; twice daily; 7 days) leads to significant neuroprotection, however, it displays a bell-shaped neuroprotective profile, being ineffective at high doses in 6-OHDA rat model of Parkinson disease (PD).

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[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

In Vitro: H₂O : 100 mg/mL (315.16 mM; Need ultrasonic)配制储备液