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• 产品描述： 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

• 靶点： Kd: 40 nM (iNOS) IC50: 2.19 μM (human iNOS); 544 μM (human eNOS); 177 μM (human nNOS) ED50: 1.15 μM (rat iNOS); 252 μM (rat nNOS);NOS

• 体外研究：
  GW274150 inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC50 values of 0.2 μM. 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

• 体内研究：
  GW274150 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 (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. GW274150 (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). Animal Model: SD-rat Dosage: 2.5, 5 and 10 mg/kg; single dose Administration: Intraperitoneal injection 5 min before carrageenan injection Result: Exerted a protective role in an acute model of inflammation, carrageenan-induced lung injury.

• 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. 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 9. 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.

• 溶解性： Soluble  in  H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	4.56 ml	22.799 ml	45.599 ml
  5 mM	0.912 ml	4.56 ml	9.12 ml
  10 mM	0.456 ml	2.28 ml	4.56 ml
  50 mM	0.091 ml	0.456 ml	0.912 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *