| Name | GW274150 phosphate |
| Description | GW274150 phosphate is a 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). |
| In vitro | GW274150 demonstrates significant selectivity for iNOS over eNOS and nNOS, with >260-fold and 219-fold selectivity in rat tissues, and >100-fold and >80-fold selectivity in human tissues, against eNOS and nNOS, respectively. Additionally, GW274150 phosphate effectively inhibits intracellular iNOS in J774 cells in a time-dependent manner, achieving IC50 values of 0.2±0.04 μM. |
| In vivo | 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).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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 100 mg/mL (315.16 mM), Sonication is recommended.
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| Keywords | human eNOS | GW-274150 phosphate | GW-274150 Phosphate | GW274150 Phosphate | GW274150 phosphate | GW 274150 Phosphate |
| Inhibitors Related | Miconazole | Aminoguanidine hydrochloride | L-NAME hydrochloride | EIT hydrobromide | 3-Bromo-7-nitroindazole | Dexamethasone acetate | S-Methylisothiourea sulfate | Cannabigerol | 1400W dihydrochloride | Flavone | S-(2-aminoethyl) Isothiourea (dihydrobromide) | Diallyl disulfide |
United States
