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Furegrelate sodium

Names

[ CAS No. ]:
85666-17-7

[ Name ]:
Furegrelate sodium

[Synonym ]:
Sodium 5-(pyridin-3-ylmethyl)-1-benzofuran-2-carboxylate
Sodium p-Styrenesulfonate
4-Vinylbenzenesulfonic acid sodium salt
sodium styrene sulphonate
p-styrenesulfonic acid sodium salt
sodium styrene sulfonate
sodium styrene-4-sulphonate
Sodium 5-(3-pyridinylmethyl)-1-benzofuran-2-carboxylate
Styrene-4-sulfonic acid sodium salt
5-(3-Pyridinylmethyl)-2-benzofurancarboxylic Acid Sodium Salt
2-Benzofurancarboxylic acid, 5-(3-pyridinylmethyl)-, sodium salt (1:1)
sodium 4-styrenesulfonate
Sodium 4-vinylbenzenesulfonate

Biological Activity

[Description]:

Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate Sodium inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate Sodium is being developed as an antiplatelet agent[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Others >> Others

[In Vivo]

Furegrelate Sodium (U-63557A) (1-5 mg/kg; Oral) prevents blockage of the coronary artery[1]. Furegrelate Sodium (0.1-5 mg/kg; i.v.) prevents the blockage of stenosed coronary arteries caused platelet aggregation[1]. Furegrelate Sodium blunts the development of hypoxia-induced pulmonary arterial hypertension (PAH) in an established neonatal piglet model primarily by preserving the structural integrity of the pulmonary vasculature[2]. Furegrelate also is orally available, has a long half-life of 4.2–5.8 hours in adult humans (compared to several other therapies for PAH including nitric oxide and prostacyclin analogs), and reportedly is highly specific for its target enzyme[2]. Animal Model: Mongrel dogs (19-30 kg)[1] Dosage: 1-5 mg/kg Administration: Oral (via a gastric tube) Result: Prevented blockage of the coronary artery.

[References]

[1]. Gorman RR, et al. Inhibition of platelet thromboxane A2 synthase activity by sodium 5-(3'-pyridinylmethyl)benzofuran-2-carboxylate. Prostaglandins. 1983 Aug;26(2):325-42.

[2]. Hirenallur-S DK, et al. Furegrelate, a thromboxane synthase inhibitor, blunts the development of pulmonary arterial hypertension in neonatal piglets. Pulm Circ. 2012 Apr-Jun;2(2):193-200.

Chemical & Physical Properties

[ Boiling Point ]:
458.7ºC at 760 mmHg

[ Molecular Formula ]:
C15H10NNaO3

[ Molecular Weight ]:
275.235

[ Flash Point ]:
231.2ºC

[ Exact Mass ]:
275.055847

[ PSA ]:
66.16000

[ LogP ]:
1.78210

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds