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ME-3277 是一种强效的 GPIIb/IIIa 拮抗剂。ME-3277 在兔大脑中动脉 (MCA) 光血栓闭塞模型中可减少脑梗死,且不增加颅内出血。ME-3277 可用于急性脑梗死的相关研究。

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ME-3277

ME-3277 Chemical Structure

CAS No. : 165948-72-1

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  • 生物活性

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  • 参考文献

生物活性

ME-3277 is a potent GPIIb/IIIa antagonist. ME-3277 reduces cerebral infarction without enhancing intracranial hemorrhage in photothrombotic occlusion of rabbit middle cerebral artery (MCA). ME-3277 can be used for the acute cerebral infarction research[1].

IC50 & Target[1]

GPIIb/IIIa

 

体内研究
(In Vivo)

ME-3277 (0.15、0.3 和 0.6 mg/kg ,静脉推注,随后以 0.125、0.25 和 0.5 mg/kg/h 的速度静脉输注,在光化学反应后 30 分钟开始,持续 24 小时) 在兔大脑中动脉 (MCA) 光化学血栓闭塞模型中,能够减少脑梗死范围且不加剧颅内出血[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rabbits (2-3 kg) induced by photochemical reaction[1]
Dosage: 0.15, 0.3, and 0.6 mg/kg bolus, followed by 0.125, 0.25, and 0.5 mg/kg/h infusion
Administration: i.v., 30 min post-photochemical reaction for 24 h
Result: Inhibited ex vivo platelet aggregation significantly and maintained through the 24-hour period, with inhibition ratios of approximately 60, 80, and 90% at low, middle, and high doses, respectively.
Prolonged bleeding time at 2 or 24 hours after the photochemical reaction but by less than 2-fold at low dose.
Significantly prolonged the bleeding time by about 3-fold at both 2 hours and 24 hours at high dose.
Increased the total reflow time in a dose-dependent manner.
Significantly increased the total reflow time (31.7% vs. 3.8% in vehicle) and had a tendency to improve the 24 hours patency at high dose.
Significantly decreased the neurologic score to 3.5 at a low dose, 4.5 at a middle dose, and 3.5 at a high dose, respectively.
Decreased the infarct volume of total and cerebral cortex area to 13.1% and 4.7% at a low dose, 16.4% and 7.1% at a middle dose, and 12.9% and 5.2% at a high dose, respectively.
Significantly decreased the hemorrhagic volume.
The hemorrhage volume normalized to infarct volume did not differ significantly among the treatment groups and the vehicle control group.
分子量

448.45

Formula

C20H20N2O8S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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ME-3277
目录号:
HY-19248
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