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71079-19-1

中文名稱 替美該定
英文名稱 Timegadine
CAS 71079-19-1
分子式 C20H23N5S
分子量 365.5
MOL 文件 71079-19-1.mol
71079-19-1 結(jié)構(gòu)式 71079-19-1 結(jié)構(gòu)式

基本信息

中文別名
替美加定
替美該定
N-環(huán)己基-N''-(2-甲基喹啉-4-基)-N'-2-噻唑基胍
英文別名
SR1368
Timegadine
N-Cyclohexyl-N''-(2-methylquinol-4-yl)-N'-2-thiazolylguanidine
N-Cyclohexyl-N'-(2-methyl-4-quinolyl)-N''-(2-thiazolyl)guanidine
Guanidine, N-cyclohexyl-N'-(2-methyl-4-quinolinyl)-N''-2-thiazolyl-

物理化學(xué)性質(zhì)

沸點(diǎn)550.8±52.0 °C(Predicted)
密度1.31±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)7.71±0.50(Predicted)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
Timegadine 是一種新的抗炎藥,被發(fā)現(xiàn)是一種有效的競爭性前列腺素合成酶抑制劑,同時也能抑制環(huán)加氧酶和脂氧合酶。
靶點(diǎn)

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)

體外研究

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.

體內(nèi)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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