Dazoxiben hydrochloride is a potent, orally active thromboxane (TX) synthase inhibitor that reduces the formation of blood clots. 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. In vivo, Dazoxiben (100 μg/kg, intraperitoneal administration) produces a marked prolongation of the tail bleeding time with 96.8 ± 10.8 secs.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 30 mg/mL|
Pharmacological characterization of cinnamophilin, a novel dual inhibitor of thromboxane synthase and thromboxane A2 receptor.
Yu SM, et al. Br J Pharmacol. 1994 Mar;111(3):906-12. PMID: 8019768.
Differential effects of dazoxiben, a selective thromboxane-synthase inhibitor, on platelet and renal prostaglandin-endoperoxide metabolism.
Patrignani P, et al. J Pharmacol Exp Ther. 1984 Feb;228(2):472-7. PMID: 6537977.
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