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GW274150
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
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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $32 | In Stock | |
| 5 mg | $73 | In Stock | |
| 10 mg | $123 | In Stock | |
| 25 mg | $255 | In Stock | |
| 50 mg | $413 | In Stock | |
| 100 mg | $662 | In Stock |
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Purity:96.43%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 & Solubility Information
| 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 | ||||||||||||||||||||||||||||||||||||
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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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
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 (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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