产品
编 号：F270245
分子式：C8H17N3O2S
分子量：219.3
分子式：C8H17N3O2S
分子量：219.3
产品类型
规格
价格
是否有货
5mg
1350
In-stock
10mg
2250
In-stock
25mg
4650
In-stock
50mg
7500
In-stock
100mg
12000
In-stock
结构图
CAS No: 210354-22-6
产品详情
生物活性：
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.
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.
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.
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.
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.
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.
产品资料
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