Description
| 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. |
| Targets&IC50 | TXA2 receptor:apr 10 nM, TXA2 synthase:appr 10 nM |
| 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.) is rapidly and well (90%) absorbed with a systemic availability of about 30% in rats. Terbogrel (0.1-3.0 mg/kg) shows an impressive antithrombotic efficacy in rabbits.[2] |
| Synonyms | BIBV 308SE |
| Molecular Weight |
405.49 |
| Formula | C23H27N5O2 |
| CAS No. | 149979-74-8 |
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 27.5 mg/mL (67.82 mM)
