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GW274150 phosphate

Catalog No. T11518   CAS 438542-15-5

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).

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GW274150 phosphate Chemical Structure
GW274150 phosphate, CAS 438542-15-5
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Solubility Information

H2O: 100 mg/mL (315.16 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Alderton WK, et al. GW274150 and GW273629 are potent and highly selective inhibitors of inducible nitric oxide synthase in vitro and in vivo.Br J Pharmacol. 2005 Jun;145(3):301-12. 2. Dugo L, et al. Effects of GW274150, a novel and selective inhibitor of iNOS activity, in acute lung inflammation. Br J Pharmacol. 2004 Mar;141(6):979-87. Epub 2004 Feb 3. Broom L, et al. Neuroprotection by the selective iNOS inhibitor GW274150 in a model of Parkinson disease.Free Radic Biol Med. 2011 Mar 1;50(5):633-40.

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Keywords

GW274150 phosphate 438542-15-5 Immunology/Inflammation NOS GW274150 Phosphate GW-274150 Phosphate GW-274150 phosphate GW 274150 Phosphate inhibitor inhibit

 

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