GW274150
Based on 2 publication(s) in Google Scholar
GW274150 is a potent, 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). GW274150 also displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 exerts a protective role in an acute model of lung injury inflammation.
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- Pureza: 98.42%
- No. CAS: 210354-22-6
- Fòrmula: C8H17N3O2S
- Peso molecular:219.30
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) GW274150
More
Actividad biológica
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iNOS |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DLD-1 | IC50 |
220 nM
Compound: 2, GW-274150
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Inhibition of human iNOS expressed in human DLD1 cells after 1 hr
Inhibition of human iNOS expressed in human DLD1 cells after 1 hr
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[PMID: 18024030] |
| Sf9 | IC50 |
8400 nM
Compound: 2, GW-274150
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Inhibition of human nNOS expressed in insect SF9 cells after 1 hr
Inhibition of human nNOS expressed in insect SF9 cells after 1 hr
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[PMID: 18024030] |
GW274150 inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC50 values of 0.2 μM[1].GW274150 is >260-fold and 219-fold selective for iNOS against eNOS and nNOS in rat tissues, respectively. And it displays >100-fold and >80-fold for human iNOS against human eNOS and nNOS, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD-rat[2]
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Dosage:2.5, 5 and 10 mg/kg; single dose
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Administration:Intraperitoneal injection 5 min before carrageenan injection
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Result:Exerted a protective role in an acute model of inflammation, carrageenan-induced lung injury.
Chemical Information
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No. CAS 210354-22-6
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Appearance Solid
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Peso molecular 219.30
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Fòrmula C8H17N3O2S
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Color White to off-white
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SMILES
N[C@@H](CCSCCNC(C)=N)C(O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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EMBO Mol Med
Pharmacological or genetic inhibition of iNOS prevents cachexia-mediated muscle wasting and its associated metabolism defects. [Abstract]2021 Jul 7;13(7):e13591. PMID: 34096686 -
Solvente y solubilidad
H2O : ≥ 62 mg/mL (282.72 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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 [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 4.5600 mL | 22.7998 mL | 45.5996 mL | 113.9991 mL |
| 5 mM | 0.9120 mL | 4.5600 mL | 9.1199 mL | 22.7998 mL | |
| 10 mM | 0.4560 mL | 2.2800 mL | 4.5600 mL | 11.3999 mL | |
| 15 mM | 0.3040 mL | 1.5200 mL | 3.0400 mL | 7.5999 mL | |
| 20 mM | 0.2280 mL | 1.1400 mL | 2.2800 mL | 5.7000 mL | |
| 25 mM | 0.1824 mL | 0.9120 mL | 1.8240 mL | 4.5600 mL | |
| 30 mM | 0.1520 mL | 0.7600 mL | 1.5200 mL | 3.8000 mL | |
| 40 mM | 0.1140 mL | 0.5700 mL | 1.1400 mL | 2.8500 mL | |
| 50 mM | 0.0912 mL | 0.4560 mL | 0.9120 mL | 2.2800 mL | |
| 60 mM | 0.0760 mL | 0.3800 mL | 0.7600 mL | 1.9000 mL | |
| 80 mM | 0.0570 mL | 0.2850 mL | 0.5700 mL | 1.4250 mL | |
| 100 mM | 0.0456 mL | 0.2280 mL | 0.4560 mL | 1.1400 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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