化合物 T11518L
- CAS号:210354-22-6
- 英文名:(S)-2-AMINO-(1-IMINOETHYLAMINO)-5-THIOHEPTANOIC ACID
- 中文名:化合物 T11518L
- CBNumber:CB3116696
- 分子式:C8H17N3O2S
- 分子量:219.3
- MOL File:Mol file
- 沸点 :392.3±52.0 °C(Predicted)
- 密度 :1.30±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 形态 :Solid
- 酸度系数(pKa) :2.22±0.10(Predicted)
- 颜色 :White to off-white
- 水溶解性 :Water : ≥ 62 mg/mL (282.72 mM)
化合物 T11518L性质、用途与生产工艺
- 生物活性 GW274150 是一种有效的，选择性的，口服活性的 NADPH 依赖型人一氧化氮合成酶 (iNOS) (Kd=40 nM) 和大鼠诱导型一氧化氮合酶 (iNOS) 抑制剂。GW274150 对人和大鼠的内皮一氧化氮合酶 (eNOS) 和神经元一氧化氮合酶 (nNOS) 均显示较低效力。GW274150 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 inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC 50 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.
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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 (ED 50 =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.
- 更新日期：2024/11/08
- 产品编号：HY-12119
- 产品名称：化合物 T11518L GW274150
- CAS编号：210354-22-6
- 包装：5mg
- 价格：900元
- 更新日期：2024/11/08
- 产品编号：HY-12119
- 产品名称：化合物 T11518L GW274150
- CAS编号：210354-22-6
- 包装：10mM * 1mLin Water
- 价格：990元
- 公司名称：CLEARSYNTH LABS LTD.
- 联系电话：--
- 电子邮件：sales@clearsynth.com
- 国家：印度
- 产品数：6257
- 优势度：58
