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210354-22-6

中文名称 化合物 T11518L
英文名称 (S)-2-AMINO-(1-IMINOETHYLAMINO)-5-THIOHEPTANOIC ACID
CAS 210354-22-6
分子式 C8H17N3O2S
分子量 219.3
MOL 文件 210354-22-6.mol
更新日期 2024/05/28 11:40:32
210354-22-6 结构式 210354-22-6 结构式

基本信息

中文别名
乙酰基半胱氨酸杂质4
化合物 T11518L
4-(2-ACETAMIDOETHYLSULFANYL)-2-AMINOBUTANOIC ACID
英文别名
GW274150
GW274150 (GW-274150
Acetylcysteine Impurity 4
4-(2-acetamidoethylthio)-2-aminobutanoic acid
S-[2-[(1-iminoethyl)amino]ethyl]-L-Homocysteine
4-(2-acetamidoethylsulfanyl)-2-aminobutanoicacid
L-Homocysteine, S-[2-[(1-iminoethyl)amino]ethyl]-
(S)-2-AMINO-(1-IMINOETHYLAMINO)-5-THIOHEPTANOIC ACID

物理化学性质

沸点392.3±52.0 °C(Predicted)
密度1.30±0.1 g/cm3(Predicted)
储存条件-20°C储存
酸度系数(pKa)2.22±0.10(Predicted)
水溶解性Water : ≥ 62 mg/mL (282.72 mM)
化合物 T11518L价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-12119化合物 T11518L
GW274150
210354-22-65mg900元
2024/04/30HY-12119化合物 T11518L
GW274150
210354-22-610mM * 1mLin Water990元
2024/04/30HY-12119化合物 T11518L
GW274150
210354-22-610mg1500元

常见问题列表

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。
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)

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.

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.
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