127654-03-9
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- CAS号:
- 127654-03-9
- 英文名:
- KF 13218
- 英文别名:
- KF 13218;Hexanoic acid, 6-(5,6-dihydro-6-methyl-5-oxo-11H-pyrido[4,3-c][1]benzazepin-11-ylidene)-, (6Z)-
- 中文名:
- 127654-03-9
- 中文别名:
- 化合物 T11755
- CBNumber:
- CB11306036
- 分子式:
- C20H20N2O3
- 分子量:
- 336.38
- MOL File:
- 127654-03-9.mol
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127654-03-9化学性质
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沸点:
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576.2±50.0 °C(Predicted)
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密度:
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1.281±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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4.71±0.10(Predicted)
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127654-03-9性质、用途与生产工艺
KF 13218 是一种有效和持久的选择性血栓烷 B2 (TXB2) 合成酶抑制剂,IC50 值为 5.3±1.3 nM。
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.
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.
127654-03-9
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127654-03-9, 127654-03-9 相关搜索:
- 对照品
- 化合物 T11755
- 127654-03-9
- Hexanoic acid, 6-(5,6-dihydro-6-methyl-5-oxo-11H-pyrido[4,3-c][1]benzazepin-11-ylidene)-, (6Z)-
- KF 13218