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Description | GW274150 is an orally active, selective and potent dual inhibitor of NADPH-dependent human nitric oxide synthase (iNOS) (Kd=40 nM) and rat inducible nitric oxide synthase (iNOS).GW274150 has a low activity against endothelial nitric oxide synthase (eNOS) and neuronal nitric oxide synthase (nNOS) in humans and rats. GW274150 showed protective effects in an inflammatory model of acute lung injury. |
Targets&IC50 | nNOS (rat):252 μM(ED50), iNOS (human):2.19 μM(kd), iNOS (rat): 1.15 μM(ED50), eNOS (human):544 μM(kd), nNOS (human):177 μM(kd), iNOS (rat):1.15 μM(ED50), iNOS:(kd)40 nM, iNOS:40 nM(kd) |
In vitro | GW274150 inhibits intracellular iNOS in J774 cells with an IC50 of 0.2 μM and demonstrates >260-fold and 219-fold selectivity for eNOS and nNOS, respectively, in rat tissue, as well as >100-fold and >80-fold selectivity for human eNOS and nNOS, respectively.[1] |
In vivo | GW274150 is a long-acting (half-life in rats is 5 hours) iNOS inhibitor, which can inhibit the LPS-mediated increase in plasma NO2- and NO3- levels 14 h after a single intraperitoneal administration (ED50=3 mg/kg ).[2] GW274150 (2.5, 5, and 10 mg/kg; i.p.; before carrageenan injection; SD rats) reduces the extent of carrageenan-induced lung injury in a dose-related manner. Pleural cavity edema formation and PMN infiltration were also significantly attenuated in a dose-related manner in rats.[2] GW274150 (30 mg/kg; oral; twice daily; 7 days; SD rats) resulted in significant neuroprotection, however, it showed bell-shaped neuroprotection in 6-OHDA rats with Parkinson's disease (PD) Ineffective at high doses in the model.[3] |
Molecular Weight | 219.3 |
Formula | C8H17N3O2S |
Cas No. | 210354-22-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: < 1 mg/mL (insoluble or slightly soluble) H2O: 50 mg/mL (228 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O
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