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GW274150

🥰Excellent
Catalog No. T11518LCas No. 210354-22-6

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.

GW274150

GW274150

🥰Excellent
Purity: 99.90%
Catalog No. T11518LCas No. 210354-22-6
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.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$32In StockIn Stock
5 mg$73In StockIn Stock
10 mg$123In StockIn Stock
25 mg$255In StockIn Stock
50 mg$413In StockIn Stock
100 mg$662In Stock-
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Purity:99.90%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
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
eNOS (human):544 μM(kd), nNOS (rat):252 μM(ED50), iNOS (human):2.19 μM(kd), iNOS:(kd)40 nM, iNOS:40 nM(kd), nNOS (human):177 μM(kd), iNOS (rat): 1.15 μM(ED50), iNOS (rat):1.15 μM(ED50)
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]
Chemical Properties
Molecular Weight219.3
FormulaC8H17N3O2S
Cas No.210354-22-6
SmilesC([C@@H](C(O)=O)N)CSCCNC(C)=N
Relative Density.1.30 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: < 1 mg/mL (insoluble or slightly soluble)
H2O: 50 mg/mL (228 mM), Sonication is recommended.
Solution Preparation Table
H2O
1mg5mg10mg50mg
1 mM4.5600 mL22.7998 mL45.5996 mL227.9982 mL
5 mM0.9120 mL4.5600 mL9.1199 mL45.5996 mL
10 mM0.4560 mL2.2800 mL4.5600 mL22.7998 mL
20 mM0.2280 mL1.1400 mL2.2800 mL11.3999 mL
50 mM0.0912 mL0.4560 mL0.9120 mL4.5600 mL
100 mM0.0456 mL0.2280 mL0.4560 mL2.2800 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Keywords

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