GW274150 phosphate
Based on 2 publication(s) in Google Scholar
GW274150 phosphate 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 phosphate displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 phosphate exerts a protective role in an acute model of lung injury inflammation.
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- 純度: 98.02%
- CAS 番号: 438542-15-5
- 分子式: C8H20N3O6PS
- 分子量:317.30
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保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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溶剤 & 溶解度
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MedChemExpress（MCE）の使用を引用している文献 GW274150 phosphate
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生物活性
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iNOS |
GW274150 phosphate inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC50 values of 0.2±0.04 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
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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.
化学情報
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CAS 番号 438542-15-5
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性状 Solid
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分子量 317.30
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分子式 C8H20N3O6PS
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Color White to off-white
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SMILES
CC(NCCSCC[C@H](N)C(O)=O)=N.O=P(O)(O)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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 -
溶剤 & 溶解度
H2O : 100 mg/mL (315.16 mM; Need ultrasonic)
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 12.5 mg/mL (39.39 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
純度とドキュメンテーション
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データシート (275 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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取扱説明書 (2659 KB)
参考文献
[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 | 3.1516 mL | 15.7580 mL | 31.5159 mL | 78.7898 mL |
| 5 mM | 0.6303 mL | 3.1516 mL | 6.3032 mL | 15.7580 mL | |
| 10 mM | 0.3152 mL | 1.5758 mL | 3.1516 mL | 7.8790 mL | |
| 15 mM | 0.2101 mL | 1.0505 mL | 2.1011 mL | 5.2527 mL | |
| 20 mM | 0.1576 mL | 0.7879 mL | 1.5758 mL | 3.9395 mL | |
| 25 mM | 0.1261 mL | 0.6303 mL | 1.2606 mL | 3.1516 mL | |
| 30 mM | 0.1051 mL | 0.5253 mL | 1.0505 mL | 2.6263 mL | |
| 40 mM | 0.0788 mL | 0.3939 mL | 0.7879 mL | 1.9697 mL | |
| 50 mM | 0.0630 mL | 0.3152 mL | 0.6303 mL | 1.5758 mL | |
| 60 mM | 0.0525 mL | 0.2626 mL | 0.5253 mL | 1.3132 mL | |
| 80 mM | 0.0394 mL | 0.1970 mL | 0.3939 mL | 0.9849 mL | |
| 100 mM | 0.0315 mL | 0.1576 mL | 0.3152 mL | 0.7879 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.
GW274150 phosphate 関連分類
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