替美该定
| 中文名称 | 替美该定 |
|---|---|
| 中文同义词 | 替美该定;替美加定;N-环己基-N''-(2-甲基喹啉-4-基)-N'-2-噻唑基胍;化合物 T13160 |
| 英文名称 | Timegadine |
| 英文同义词 | Timegadine;N-Cyclohexyl-N'-(2-methyl-4-quinolyl)-N''-(2-thiazolyl)guanidine;N-Cyclohexyl-N''-(2-methylquinol-4-yl)-N'-2-thiazolylguanidine;SR1368;Guanidine, N-cyclohexyl-N'-(2-methyl-4-quinolinyl)-N''-2-thiazolyl- |
| CAS号 | 71079-19-1 |
| 分子式 | C20H23N5S |
| 分子量 | 365.49 |
| EINECS号 | 2751840 |
| 相关类别 | |
| Mol文件 | 71079-19-1.mol |
| 结构式 |  |
替美该定 性质
| 沸点 | 550.8±52.0 °C(Predicted) |
|---|---|
| 密度 | 1.31±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 7.71±0.50(Predicted) |
|
COX 5 nM (IC 50 , in rabbit platelets) |
COX 20 μM (IC 50 , in rat brain) |
lipo-oxygenase 100 μM (IC 50 , in horse and washed rabbit platelets) |
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of of COX and lipo-oxygenase, with IC 50 s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of prostaglandin synthetase which also inhibits cyclo-oxygenase (COX) and lipoxygenase. Daily oral doses of 10 to 30 mg/kg of Timegadine significantly inhibit both the primary and secondary lesions of adjuvant arthritis when the treatment is initiated on the day of the disease induction and continues for 28 days. Timegadine is able specifically to prevent the development of the swelling of the non-injected paw until 28 days after the adjuvant injection when administered for 5 days prior to and 5 days after the induction of the disease, in analogy with the effect of cyclophosphamide.