货号:A662355 同义名: 盐酸替罗非班 一水合物 / L700462 hydrochloride monohydrate;MK383 hydrochloride monohydrate
Tirofiban HCl H2O is a non-peptide reversible antagonist of the platelet integrin glycoprotein (GP) IIb/IIIa receptor used as an antiplatelet drug.
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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 |
++++
αvβ5 receptor, IC50: 0.3 nM αvβ3 receptor, IC50: 1.2 nM |
98+% | |||||||||||||||||
Lifitegrast | ✔ | 97% | |||||||||||||||||
Cilengitide TFA |
+++
αvβ5 receptor, IC50: 79 nM αvβ3 receptor, IC50: 4.1 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 | The binding of glycoprotein (GP) IIb/IIIa receptor to fibrinogen is a prerequisite in platelet activation and aggregation. Tirofiban Hydrochloride Monohydrate is the hydrochloride monohydrate form of Tirofiban. Tirofiban is a potent GPIIb/IIIa antagonist. It inhibited the aggregation of in vitro human gel-filtered platelets induced by ADP, collagen, gamma-thrombin, and U46619 with IC50 values ranging from 12 nM to 31 nM. It also displayed inhibitory activity against human PRP platelet aggregation induced by ADP, collagen, gamma-thrombin, U46619, epinephrine, and arachidonic acid with IC50 values ranging from 31 nM to 66 nM. Tirofiban inhibited the platelet aggregation in human, rhesus monkey, and dog whole blood with IC50 values of 81, 140, and 353 nM, respectively. The intravenous administration of tirofiban (1 mg/kg) in dogs significantly inhibited ex vivo ADP-induced platelet aggregation in platelet-rich plasma (PRP) and the prolongation of template bleeding time. Continuous infusions of tirofiban (0.1-10 µg/kg/min) inhibited ex vivo platelet aggregation in PRP induced by ADP and collagen in a dose-dependent manner. Moreover, the combined treatment with tirofiban (1µg/kg/min, i.v., 120min) and ticlopidine (20 mg/kg/day, p.o., 4 days) in dogs did not change the pharmacokinetic profile of tirofiban nor the platelet count[3]. |
Dose | Rat: 1 mg/kg - 20 mg/kg[3] (i.v.) Dog: 0.12 mg/kg - 3.6 mg/kg[3] (i.v.) |
Administration | i.v. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01087723 | Acute Coronary Syndrome | Phase 3 | Completed | - | - |
NCT01087723 | - | 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 |
2.02mL 0.40mL 0.20mL |
10.10mL 2.02mL 1.01mL |
20.20mL 4.04mL 2.02mL |
CAS号 | 150915-40-5 |
分子式 | C22H39ClN2O6S |
分子量 | 495.073 |
别名 | 盐酸替罗非班 一水合物 ;L700462 hydrochloride monohydrate;MK383 hydrochloride monohydrate;Tirofiban (hydrochloride hydrate);MK-383 Hydrochloride;Tirofiban Hydrochloride |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
DMSO: 105 mg/mL(212.09 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 |
动物实验配方 |
PO 0.5% CMC-Na 31 mg/mL suspension |