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GW274150 phosphate

Catalog No. T11518Cas No. 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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Pack Size	Price	Availability	Quantity
2 mg	$48	5 days

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Product Introduction

Bioactivity

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.

Chemical Properties

Molecular Weight	317.3
Formula	C8H20N3O6PS
Cas No.	438542-15-5

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 100 mg/mL (315.16 mM)

Solution Preparation Table

H2O

	1mg	5mg	10mg	50mg
1 mM	3.1516 mL	15.7580 mL	31.5159 mL	157.5796 mL
5 mM	0.6303 mL	3.1516 mL	6.3032 mL	31.5159 mL
10 mM	0.3152 mL	1.5758 mL	3.1516 mL	15.7580 mL
20 mM	0.1576 mL	0.7879 mL	1.5758 mL	7.8790 mL
50 mM	0.0630 mL	0.3152 mL	0.6303 mL	3.1516 mL
100 mM	0.0315 mL	0.1576 mL	0.3152 mL	1.5758 mL

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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