149979-74-8
基本信息
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)-
物理化学性质
| 沸点 | 613.5±65.0 °C(Predicted) |
| 密度 | 1.13±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 4.66±0.10(Predicted) |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P305+P351+P338 |
常见问题列表
IC50: apr 10 nM (thromboxane A2 receptor), appr 10 nM (thromboxane A2 synthase)
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.
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.