Bioactivity | 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]. |
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: |
Name | Furegrelate sodium |
CAS | 85666-17-7 |
Formula | C15H10NNaO3 |
Molar Mass | 275.23 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [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. |