| Description | Terbogrel is an oral thromboxane A2 receptor antagonist (IC50 is about 10 nM) and thromboxane A2 synthase inhibitor (IC50 is about 10 nM). Terbogrel is an antiplatelet compound that inhibits platelet aggregation and is a potential compound for the prevention of blood clots. |
| In vitro | Terbogrel inhibits collagen-induced platelet aggregation in human platelet-rich plasma and whole blood (IC50: 310 ± 18 nM (n = 8) and 52 ± 20 nM (n = 6), respectively). Terbogrel (1 μM) fully inhibits U46619-induced platelet aggregation (IC50: 10 nM). 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 blocks the thromboxane A2/endoperoxide receptor on washed human platelets (IC50: 11 ± 6 nM (n = 2) and IC50: 38 ± 1 nM (n = 15) in platelet-rich plasma).[1][2] |
| In vivo | Terbogrel（10 mg/kg，p.o.）在大鼠体内的吸收迅速且良好（90%），系统可用性约为30%。在兔子中，Terbogrel（0.1-3.0 mg/kg）展示了显著的抗血栓效果。[2] |
| Target activity | TXA2 receptor:apr 10 nM, TXA2 synthase:appr 10 nM |
| Synonyms | BIBV 308SE |
| molecular weight | 405.49 |
| Molecular formula | C23H27N5O2 |
| CAS | 149979-74-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 27.5 mg/mL (67.82 mM) |
| References | 1. Muck S, et al. Effects of terbogrel on platelet function and prostaglandin endoperoxide transfer. Eur J Pharmacol. 1998;344(1):45-48. 2. Soyka R, et al. Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors. J Med Chem. 1999;42(7):1235-1249. |