Furegrelate (sodium salt) (Synonyms: U-63557A) |
Catalog No.GC13536 |
Le furegrelate sodique (U-63557A) est un inhibiteur puissant, disponible par voie orale et sélectif de la thromboxane synthase.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 85666-17-7
Sample solution is provided at 25 µL, 10mM.
Furegrelate (sodium salt) is a potent inhibitor of thromboxane synthase [1][2].
Thromboxane A synthase 1 (platelet, cytochrome P450, family 5, subfamily A) is a cytochrome P450 enzyme that catalyzes the conversion of prostaglandin H2 to thromboxane A2. Thromboxanes play an important role in vasoconstriction and platelet aggregation.
Furegrelate (sodium salt), also known as sodium 5-(3'-pyridinylmethyl)benzofuran-2-carboxylate (U-63557A), is a potent, specific and orally available thromboxane synthase inhibitor. U-63557A is a potent inhibitor of the thromboxane synthase in human platelets in vitro, as well as in rhesus monkey platelets ex vivo. U-63557A didn’t inhibit thrombin-stimulated PGI2 biosynthesis in human endothelial cells, the 5-lipoxygenase in human neutrophils, or the cyclooxygenase in a variety of test systems [2].
In rhesus monkeys, U-63557A inhibited the platelet thromboxane synthase by approximately 80% for at least 12 hrs. In anesthetized dogs, U-63557A inhibited the blockage of stenosed coronary arteries caused platelet aggregation. While the protective effects of U-63557A could be reversed by cyclooxygenase inhibitors. U-63557A is a promising compound for the evaluation of the role of thromboxane synthase in a variety of pathophysiological states [2].
References:
[1]. Johnson RA, Nidy EG, Aiken JW, et al. Thromboxane A2 synthase inhibitors. 5-(3-Pyridylmethyl)benzofuran-2-carboxylic acids. J Med Chem. 1986 Aug;29(8):1461-8.
[2]. Gorman RR, Johnson RA, Spilman CH, et al. Inhibition of platelet thromboxane A2 synthase activity by sodium 5-(3'-pyridinylmethyl)benzofuran-2-carboxylate. Prostaglandins. 1983 Aug;26(2):325-42.
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