CAS:101001-34-7Ethyl 2-(2-(4,5-bis(4-methoxyphenyl)thiazol-2-yl)-1H-pyrrol-1-yl)acetate

Synonyms: Pamicogrel

KBT3022 is a COX inhibitor.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

101001-34-7

储存条件

分子式

C25H24N2O4S

运输

蓝冰

分子量

448.53

别名

Pamicogrel

溶解度

动物实验配方

生物活性

描述Platelet activation, adhesion and aggregation play a pivotal role in the pathogenesis of arterial thrombosis. Antiplatelet agents exert their ability to inhibit platelet cyclooxygenase, thus preventing the formation of thromboxane A₂, a potent platelet activator and vasoconstrictor^[1]. KBT-3022, a new antiplatelet agent, inhibits COX from ovine seminal gland with an IC₅₀ value of 0.69 μM^[2]. In vitro, KBT-3022 (100 μM) and its metabolite desethyl KBT-3022 (10 and 100 μM) inhibited arachidonic acid-induced swelling of guinea pig cortical slices. KBT-3022 (3-100 μM) and desethyl KBT-3022 (3-30 μM) inhibited lipid peroxidation in guinea pig brain homogenate. In vivo, oral administration of KBT-3022 (1, 3 and 10 mg/kg) and indomethacin (10 and 30 mg/kg) prevented brain edema induced by bilateral carotid occlusion and recirculation in gerbils. KBT-3022 (10 mg/kg) inhibited lactate accumulation in gerbil brain after ischemia and recirculation. These results suggest that KBT-3022 prevents development of both cytotoxic edema in vitro and vasogenic edema in vivo^[3].