GW274150 PHOSPHATE
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- CAS号:
- 438542-15-5
- 英文名:
- GW274150 phosphate
- 英文别名:
- GW274150 phosphate;GW-274150 phosphate,GW274150 phosphate
- 中文名:
- GW274150 PHOSPHATE
- 中文别名:
- 化合物 T11518;GW274150 PHOSPHATE
- CBNumber:
- CB58035397
- 分子式:
- C8H20N3O6PS
- 分子量:
- 317.3
- MOL File:
- 438542-15-5.mol
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GW274150 PHOSPHATE化学性质
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储存条件:
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Store at -20°C
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形态:
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Solid
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颜色:
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White to off-white
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水溶解性:
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Water: 100 mg/mL (315.16 mM)
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GW274150 PHOSPHATE性质、用途与生产工艺
GW274150 phosphate 是一种有效的,选择性的,口服活性的 NADPH 依赖型人诱导型一氧化氮合成酶 (iNOS) (Kd=40 nM) 和大鼠 (iNOS) 抑制剂。GW274150 phosphate 对人和大鼠内皮一氧化氮合酶 (eNOS) 和神经元一氧化氮合酶 (nNOS) 均显示较低效力。GW274150 phosphate 在急性肺损伤炎症模型中发挥保护作用。
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)
GW274150 phosphate inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC
50
values of 0.2±0.04 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 phosphate is a long-acting (5 h half‐life in rats) iNOS inhibitor and is able to inhibit LPS‐mediated increase in plasma NO2
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, NO3
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levels 14 h after single intraperitoneal dose (ED
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=3 mg/kg).GW274150 phosphate (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 phosphate (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:
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SD rat
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Dosage:
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2.5, 5 and 10 mg/kg
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Administration:
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Intraperitoneal injection 5 min before carrageenan injection
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Result:
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Exerted a protective role in an acute model of inflammation, carrageenan-induced lung injury.
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GW274150 PHOSPHATE
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更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-12119A | GW274150 PHOSPHATE GW274150 phosphate | 438542-15-5 | 5mg | 900元 |
2024/04/30 | HY-12119A | GW274150 PHOSPHATE GW274150 phosphate | 438542-15-5 | 10mg | 1500元 |
438542-15-5, GW274150 PHOSPHATE 相关搜索:
- 化合物 T11518
- GW274150 PHOSPHATE
- 438542-15-5
- GW-274150 phosphate,GW274150 phosphate
- GW274150 phosphate