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CAS No.: 101001-34-7

Pamicogrel/帕米格雷 Catalog No. CSN25653

Synonyms: KBT3022;帕米格雷

KBT3022 is a COX inhibitor.

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生物活性

实验方案

技术信息

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].
参考文献

[1] Shimazawa M, Takiguchi Y, Umemura K, Kondo K, Nakashima M. Antithrombotic effects in a rat model of aspirin-insensitive arterial thrombosis of desethyl KBT-3022, the main active metabolite of a new antiplatelet agent, KBT-3022. Eur J Pharmacol. 1997;328(2-3):183-189
[2] Matsuo K, Yokota K, Yamashita A, Oda M. The mechanism of action of KBT-3022, a new antiplatelet agent. Gen Pharmacol. 1997;28(2):229-235
[3] Yamamoto N, Yokota K, Yamashita A, Oda M. Effect of KBT-3022, a new cyclooxygenase inhibitor, on experimental brain edema in vitro and in vivo. Eur J Pharmacol. 1996;297(3):225-231

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2295 mL
- 11.1474 mL
- 22.2948 mL
- 5 mM
- 0.4459 mL
- 2.2295 mL
- 4.4590 mL
- 10 mM
- 0.2229 mL
- 1.1147 mL
- 2.2295 mL

技术信息

CAS号

101001-34-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H24N2O4S

运输

蓝冰

分子量

448.53

别名

KBT3022;帕米格雷

溶解度

DMSO	45.0 mg/mL (100.3 mM)
Water	Insoluble
Ethanol	Insoluble

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