替美该定
- CAS号:71079-19-1
- 英文名:Timegadine
- 中文名:替美该定
- CBNumber:CB9875632
- 分子式:C20H23N5S
- 分子量:365.49
- MOL File:71079-19-1.mol
- 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 :Soluble in DMSO
- 酸度系数(pKa) :7.71±0.50(Predicted)
替美该定性质、用途与生产工艺
- 生物活性 Timegadine 是一种新的抗炎药,被发现是一种有效的竞争性前列腺素合成酶抑制剂,同时也能抑制环加氧酶和脂氧合酶。
-
靶点
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)
-
体外研究
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.
-
体内研究
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.
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