Eptifibatide
产品说明书
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同义名 : | - |
| CAS号 : | 188627-80-7 | |
| 货号 : | A135064 | |
| 分子式 : | C35H49N11O9S2 | |
| 纯度 : | 98% | |
| 分子量 : | 831.96 | |
| MDL号 : | MFCD05662245 | |
| 存储条件： |
Pure form Sealed in dry, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 250 mg/mL(300.49 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 50 mg/mL(60.1 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Glycoprotein (GP) IIb/IIIa complexe is responsible for the formation of platelet aggregates and the adhesion of platelets to uncovered collagen fibers in the injured vessel wall. Eptifibatide is a potent antagonist of GPIIb/IIIa complex. It dose-dependently reduced the adhesion of collagen-activated platelets to a fibrinogen-coated surface with a concentration of 4-38μg/mL and the approximate IC50 value was 11μg/mL. Eptifibatide at 4-52µg/mL reduced thrombin, collagen, and ADP-induced platelet aggregation in a concentration-dependent manner with estimated IC50 values of 16, 25, and 27µg/mL for ADP, collagen and thrombin, respectively. In addition, eptifibatide at 52µg/mL reduced lysosome secretion induced by ADP, collagen and thrombin by 70, 60, and 50 %, respectively[4]. Eptifibatide binds to GPIIb/IIIa complex with an KD value of 120nM[5]. In a mouse model of cecal slurry-induced sepsis, intravenous administration of eptifibatide (15µg/g, three times) resulted in lower sepsis scores and better survival when compared with vehicle-treated group. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01994941 | Acute Coronary Syndrome | Phase 4 | Completed | - | Hong Kong ... 展开 >> Department of Medicine, the University of Hong Kong, Queen Mary Hospital, Hospital Authority Hong Kong, Hong Kong 收起 << |
| NCT01087723 | Acute Coronary Syndrome | Phase 3 | Completed | - | - |
| NCT01103440 | Stable Angina | Phase 2 | Completed | - | United States, New York ... 展开 >> Mount Sinai Medical Center New York, New York, United States, 10029 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.20mL 0.24mL 0.12mL |
6.01mL 1.20mL 0.60mL |
12.02mL 2.40mL 1.20mL |
| 参考文献 |
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