Eptifibatide 是一种选择性的血小板糖蛋白 IIb/IIIa 受体拮抗剂,对血小板粘附有显著抑制作用。Eptifibatide 主要用于急性冠脉综合征的治疗和心脏介入手术中的抗血栓处理。
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产品名称 | Integrin ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tirofiban | ✔ | 99%+ | |||||||||||||||||
ATN-161 | ✔ | 98% | |||||||||||||||||
RGD | ✔ | 98% | |||||||||||||||||
A-205804 |
++
ICAM-1, IC50: 25 nM E-selectin, IC50: 20 nM |
98% | |||||||||||||||||
SB-273005 |
++++
αvβ3 receptor, IC50: 1.2 nM αvβ5 receptor, IC50: 0.3 nM |
98+% | |||||||||||||||||
Lifitegrast | ✔ | 97% | |||||||||||||||||
Cilengitide TFA |
+++
αvβ3 receptor, IC50: 4.1 nM αvβ5 receptor, IC50: 79 nM |
99%+ | |||||||||||||||||
Cyclo(-RGDfK) TFA | ✔ | 99%+ | |||||||||||||||||
Cyclo(RGDyK) trifluoroacetate |
++
αVβ3 integrin, IC50: 20 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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. |
Dose | Rat: 2 mg/ml/kg[3] (i.v.) | ||||||||||||||
Administration | i.v. | ||||||||||||||
Pharmacokinetics |
|
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 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.20mL 0.24mL 0.12mL |
6.01mL 1.20mL 0.60mL |
12.02mL 2.40mL 1.20mL |
CAS号 | 188627-80-7 |
分子式 | C35H49N11O9S2 |
分子量 | 831.96 |
SMILES Code | O=C(O)C[C@H](NC(CNC([C@H](CCCCNC(N)=N)N1)=O)=O)C(N[C@@H](CC2=CNC3=C2C=CC=C3)C(N4[C@](CCC4)([H])C(N[C@H](C(N)=O)CSSCCC1=O)=O)=O)=O |
MDL No. | MFCD05662245 |
别名 | |
运输 | 蓝冰 |
InChI Key | CZKPOZZJODAYPZ-LROMGURASA-N |
Pubchem ID | 448812 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, store in freezer, under -20°C |
溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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