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Dazoxiben

Names

[ CAS No. ]:
74226-22-5

[ Name ]:
Dazoxiben

[Synonym ]:
Dazoxiben hydrochloride
Dazoxiben HCl

Biological Activity

[Description]:

Dazoxiben is a potent and orally active thromboxane (TX) synthase inhibitor[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor
Research Areas >> Inflammation/Immunology

[Target]

Thromboxane (TX) synthase[1]


[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Boiling Point ]:
491.2ºC at 760 mmHg

[ Molecular Formula ]:
C12H13ClN2O3

[ Molecular Weight ]:
268.69600

[ Flash Point ]:
250.9ºC

[ Exact Mass ]:
268.06100

[ PSA ]:
64.35000

[ LogP ]:
2.46230

Safety Information

[ Hazard Codes ]:
Xi

Synthetic Route

Click to get detail synthetic route

Related Compounds