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95853-92-2

中文名稱 CGS 15435
英文名稱 CGS 15435
CAS 95853-92-2
分子式 C20H21ClN2O2
分子量 356.85
MOL 文件 95853-92-2.mol
95853-92-2 結構式 95853-92-2 結構式

基本信息

中文別名
化合物 T10783
化合物CGS 15435
英文別名
CGS 15435
1H-Indole-3-hexanoic acid, 5-chloro-1-methyl-2-(3-pyridinyl)-

物理化學性質

儲存條件-20°C儲存
溶解度溶于二甲基亞砜

安全數據

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
CGS 15435 是一種有效的血栓烷 (TxA2) 合成酶抑制劑,IC50 為 1 nM, 比作用于環(huán)氧合酶,PGI2 合成酶和脂氧合酶的選擇性高 100000 倍。
靶點

TXA 2

1 nM (IC 50 )

體外研究

CGS 15435 is a highly specific Tx synthetase inhibitor. CGS 15435 is only weakly effective as an inhibitor of PGE 2 (Cyclooxygenase, IC 50 =1200 μM), prostacyclin (PGI 2 synthetase, IC 50 =90 μM) or 5-Lipoxygenase (IC 50 =60 μM) product formation.

體內研究

CGS 15435 has a long duration of action, since the increases in the plasma levels of TxB 2 are prevented even at 24 h after CGS 15435 administration. CGS 15435 significantly inhibits TxB 2 formation 4, 6, 12 and 24 h after dosing. Administration of CGS 15435 0.25 or 24 h prior to Arachidonic acid (AA) produced no increase in TxB 2 in the surviving animals (4/4 and 5/6, respectively). The final TxB 2 levels in the CGS15435A (0.25 and 24 h pretreatment) groups are significantly lower (P<0.05) than those seen in the AA or the Dazoxiben (2 h pretreatment) groups.

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