中文名 | KF 13218 |
英文名 | KF 13218 |
别名 | 化合物 T11755 |
英文别名 | KF 13218 127654-03-9 Hexanoic acid, 6-(5,6-dihydro-6-methyl-5-oxo-11H-pyrido[4,3-c][1]benzazepin-11-ylidene)-, (6Z)- |
CAS | 127654-03-9 |
化学式 | C20H20N2O3 |
分子量 | 336.38 |
密度 | 1.281±0.06 g/cm3(Predicted) |
沸点 | 576.2±50.0 °C(Predicted) |
酸度系数 | 4.71±0.10(Predicted) |
存储条件 | -20℃ |
体外研究 | KF 13218 inhibits human and bovine platelet thromboxane synthase with IC 50 values of 27±5.8 nM (mean±S.E.M.) and 36±6.9 nM, respectively. KF 13218 does not inhibit cyclooxygenase or 5-lipoxygenase up to a dose of 100 μM and does not antagonize thromboxane A2/prostaglandin H2 receptors. KF 13218 inhibits arachidonic acid-induced thromboxane B2 production by human intact platelets with an IC 50 value of 5.3±1.3 nM. The IC 50 value of KF 13218 for the intact platelets is about 5 times lower than that for the microsomal enzyme. The inhibition of thromboxane synthase in platelets by KF 13218 is sustained after removal of the extracellular compound. |
体内研究 | After oral dosing in rat from 0.03 mg/kg to 3 mg/kg, KF 13218 dose-dependently inhibits the thromboxane B2 production in serum, and the inhibition is retained for 72 h. KF 13218, at a dose of 0.1 mg/kg p.o. prevents mortality induced by sodium arachidonate in rabbit. |
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