timegadine

Timegadine is a competitive inhibitor of COX and lipo-oxygenase, with IC50s 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 hydrochloride (SR1368 hydrochloride) 是 Timegadine 的盐酸盐衍生物，作为一种口服生物可利用性的 COX 和脂氧合酶 (lipo-oxygenase) 的抑制剂。它在兔血小板和大鼠脑中的 COX 的 IC50 分别为 5 nM 和 20 μM，并在马和兔血小板中的脂氧合酶呈现 IC50 为 100 μM 的抑制作用。Timegadine hydrochloride 具有抗关节炎的药理活性。