化合物 T11518L

生物活性靶点体外研究体内研究化合物 T11518L 试剂级价格

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

化合物 T11518L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 :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。
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.