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GW274150 phosphate

CAS No. : 438542-15-5

MCE 站：GW274150 phosphate

产品活性：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。

研究领域：Immunology/Inflammation

作用靶点：NO Synthase

In Vitro: 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.

In Vivo: 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 (ED₅₀=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).

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