化合物 T11518L
| 中文名称 | 化合物 T11518L |
|---|---|
| 中文同义词 | 乙酰基半胱氨酸杂质4;4-(2-ACETAMIDOETHYLSULFANYL)-2-AMINOBUTANOIC ACID;化合物 T11518L;化合物GW274150 |
| 英文名称 | (S)-2-AMINO-(1-IMINOETHYLAMINO)-5-THIOHEPTANOIC ACID |
| 英文同义词 | S-[2-[(1-iminoethyl)amino]ethyl]-L-Homocysteine;GW274150;(S)-2-AMINO-(1-IMINOETHYLAMINO)-5-THIOHEPTANOIC ACID;Acetylcysteine Impurity 4;4-(2-acetamidoethylthio)-2-aminobutanoic acid;GW274150 (GW-274150;L-Homocysteine, S-[2-[(1-iminoethyl)amino]ethyl]-;4-(2-acetamidoethylsulfanyl)-2-aminobutanoicacid |
| CAS号 | 210354-22-6 |
| 分子式 | C8H17N3O2S |
| 分子量 | 219.3 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | Mol File |
| 结构式 |  |
化合物 T11518L 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 |
| 酸度系数(pKa) | 2.22±0.10(Predicted) |
| 水溶解性 | Water : ≥ 62 mg/mL (282.72 mM) |
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 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.
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-12119 | 化合物 T11518L GW274150 | 210354-22-6 | 5mg | 900元 |
| 2024/04/30 | HY-12119 | 化合物 T11518L GW274150 | 210354-22-6 | 10mM * 1mLin Water | 990元 |