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127654-03-9

中文名稱 127654-03-9
英文名稱 KF 13218
CAS 127654-03-9
分子式 C20H20N2O3
分子量 336.38
MOL 文件 127654-03-9.mol
127654-03-9 結(jié)構(gòu)式 127654-03-9 結(jié)構(gòu)式

基本信息

中文別名
化合物 T11755
英文別名
KF 13218
Hexanoic acid, 6-(5,6-dihydro-6-methyl-5-oxo-11H-pyrido[4,3-c][1]benzazepin-11-ylidene)-, (6Z)-

物理化學(xué)性質(zhì)

沸點(diǎn)576.2±50.0 °C(Predicted)
密度1.281±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)4.71±0.10(Predicted)

常見(jiàn)問(wèn)題列表

生物活性
KF 13218 是一種有效和持久的選擇性血栓烷 B2 (TXB2) 合成酶抑制劑,IC50 值為 5.3±1.3 nM。
靶點(diǎn)

TXB 2

5.3 nM (IC 50 )

體外研究

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.

體內(nèi)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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