| Bioactivity | Dazoxiben is a potent and orally active thromboxane (TX) synthase inhibitor[1]. |
| Target | Thromboxane (TX) synthase |
| Invitro | Dazoxiben inhibits TXB2 production in clotting human whole blood with an IC50 of 0.3 μM and causes parallel enhancement of PGE2 greater than PGF2 alpha greater than 6-keto-PGF1 alpha production[1].Dazoxiben inhibits TXB2 production in rat kidney glomeruli with an IC50 of 1.60 μM) than in rat whole blood (IC50= 0.32μM), and is not associated with changes in PGE2, PGF2 alpha and 6-keto-PGF1 alpha production[1]. |
| In Vivo | Dazoxiben (intraperitoneal administration; 100 μg/kg) produces a marked prolongation of the tail bleeding time with 96.8 ± 10.8 secs[2]. |
| Name | Dazoxiben |
| CAS | 74226-22-5 |
| Formula | C12H13ClN2O3 |
| Molar Mass | 268.70 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Patrignani P, et al. Differential effects of dazoxiben, a selective thromboxane-synthase inhibitor, on platelet and renal prostaglandin-endoperoxide metabolism.J Pharmacol Exp Ther. 1984 Feb;228(2):472-7. [2]. Yu SM, et al. Pharmacological characterization of cinnamophilin, a novel dual inhibitor of thromboxane synthase and thromboxane A2 receptor.Br J Pharmacol. 1994 Mar;111(3):906-12. |