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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $48 | 5 days |
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). |
Targets&IC50 | eNOS (human):544 μM (Kd) |
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. |
Molecular Weight | 317.3 |
Formula | C8H20N3O6PS |
Cas No. | 438542-15-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 100 mg/mL (315.16 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O
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