Name | GW274150 phosphate |
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Description | 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). 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[1][2]. |
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Related Catalog | |
Target |
Kd: 40 nM (iNOS)[1] IC50: 2.19 μM (human iNOS); 544 μM (human eNOS); 177 μM (human nNOS) ED50: 1.15 μM (rat iNOS); 252 μM (rat nNOS)[1] |
In Vitro | GW274150 phosphate inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC50 values of 0.2±0.04 μM[1]. 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[1]. |
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)[2]. 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[2]. 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)[3]. Animal Model: SD rat[2] Dosage: 2.5, 5 and 10 mg/kg Administration: Intraperitoneal injection 5 min before carrageenan injection Result: Exerted a protective role in an acute model of inflammation, carrageenan-induced lung injury. |
References |
Molecular Formula | C8H20N3O6PS |
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Molecular Weight | 317.30 |