GW274150 PHOSPHATE
- CAS号:438542-15-5
- 英文名:GW274150 phosphate
- 中文名:GW274150 PHOSPHATE
- CBNumber:CB58035397
- 分子式:C8H20N3O6PS
- 分子量:317.3
- MOL File:438542-15-5.mol
- 储存条件 :Store at -20°C
- 形态 :Solid
- 颜色 :White to off-white
- 水溶解性 :Water: 100 mg/mL (315.16 mM)
GW274150 PHOSPHATE性质、用途与生产工艺
- 生物活性 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。
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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)
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体外研究
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.
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体内研究
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 - , NO3 - levels 14 h after single intraperitoneal dose (ED 50 =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: SD rat Dosage: 2.5, 5 and 10 mg/kg Administration: Intraperitoneal injection 5 min before carrageenan injection Result: Exerted a protective role in an acute model of inflammation, carrageenan-induced lung injury.
- 更新日期:2024/04/30
- 产品编号:HY-12119A
- 产品名称:GW274150 PHOSPHATE GW274150 phosphate
- CAS编号:438542-15-5
- 包装:5mg
- 价格:900元
- 更新日期:2024/04/30
- 产品编号:HY-12119A
- 产品名称:GW274150 PHOSPHATE GW274150 phosphate
- CAS编号:438542-15-5
- 包装:10mg
- 价格:1500元
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:19892
- 优势度:58
- 公司名称:Aladdin Scientific
- 联系电话:+1-+1(833)-552-7181
- 电子邮件:sales@aladdinsci.com
- 国家:美国
- 产品数:52927
- 优势度:58
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58