Bioactivity | Furegrelate (U-63557A free acid) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate is being developed as an antiplatelet agent[1][2]. |
In Vivo | Furegrelate (1-5 mg/kg;口服) 防止冠状动脉阻塞[1]。Furegrelate (0.1-5 mg/kg;静脉注射) 可防止狭窄的冠状动脉阻塞引起血小板聚集[1]。Furegrelate 主要通过保持肺血管的结构完整性来抑制缺氧诱导的新生儿仔猪肺动脉高压 (PAH) 的发展[2]。Furegrelate 与其他几种治疗 PAH 的药物相比 (包括一氧化氮和前列腺环素类似物),半衰期长;并且,Furegrelate 对靶酶具有高度特异性[2]。 |
Name | Furegrelate |
CAS | 85666-24-6 |
Formula | C15H11NO3 |
Molar Mass | 253.25 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
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. |