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149979-74-8

中文名稱 特波格雷
英文名稱 Terbogel
CAS 149979-74-8
分子式 C23H27N5O2
分子量 405.49
MOL 文件 149979-74-8.mol
149979-74-8 結(jié)構(gòu)式 149979-74-8 結(jié)構(gòu)式

基本信息

中文別名
特波格雷
英文別名
Terbogel
terbogrel
(E)-6-[3-[(N'-tert-butyl-N-cyanocarbamimidoyl)amino]phenyl]-6-pyridin-3-ylhex-5-enoic acid
5-Hexenoic acid, 6-[3-[[(cyanoamino)[(1,1-dimethylethyl)amino]methylene]amino]phenyl]-6-(3-pyridinyl)-, (5E)-

物理化學性質(zhì)

沸點613.5±65.0 °C(Predicted)
密度1.13±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)4.66±0.10(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
Terbogrel 是一種可口服的 thromboxane A2 受體拮抗劑,和 thromboxane A2 synthase 的抑制劑,IC50 值均約為 10 nM。
靶點

IC50: apr 10 nM (thromboxane A2 receptor), appr 10 nM (thromboxane A2 synthase)

體外研究

Pretreatment of platelets with terbogrel 1 μM completely inhibits thrombin-induced thromboxane A2 formation (2±1 ng/mL) but does not result in any inhibition of platelet aggregation. Terbogrel (1 μM) completely inhibits U46619-induced platelet aggregation, and the IC 50 value is 10 nM. Terbogrel inhibits both platelet aggregation and thromboxane A2 formation with an IC 50 of about 10 nM. Terbogrel inhibits the thromboxane A2 synthase in human gel-filtered platelets with an IC 50 value of 4.0 ± 0.5 nM. Terbogrel blocks the thromboxane A2/endoperoxide receptor on washed human platelets with an IC 50 of 11 ± 6 nM (n = 2) and with an IC 50 of 38 ± 1 nM (n = 15) in platelet-rich plasma. Terbogrel inhibits the collagen-induced platelet aggregation in human platelet-rich plasma and whole blood with an IC 50 of 310 ± 18 nM (n = 8) and 52 ± 20 nM (n = 6), respectively.

體內(nèi)研究

Terbogrel (0.1?3.0 mg/kg) demonstrates an impressive antithrombotic efficacy in rabbits. Terbogrel (10 mg/kg, po) is rapidly and well (90%) absorbed with a systemic availability of about 30% in rats.

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