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抑制剂描述:

产品名称:Tirofiban

产品别名:见爱必信官网

英文别名:Tirofiban

靶点:Integrin

CAS:144494-65-5

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist.

溶解性:5%TFA:3.02 mg/mL (6.85 mM)
DMSO:0.005 mg/mL (0.01 mM)

体外研究:

Tirofiban (MK-383, Aggrastat) is a nonpeptide derivative of tyrosine that selectively inhibits the GP-IIb/IIIa receptor, with minimal effects on the ɑvβ3 vitronectin receptor. It inhibits platelet aggregation of gel-filtered platelets induced by 10 μM ADP with IC50 of 9 nM, but the IC50 for inhibition of human umbilical vein adhesion to vitronectin, which depends on ɑvβ3 vitronectin receptors, is 62 μmol/L.

体内研究:Tirofiban (10 to 500 mg/kg or 360-min continuous i.v. infusions of 1 to 10 micrograms/kg/min) inhibits platelet aggregation responses to ADP and collagen in canine models. When administered to humans at 0.15μg/kg/min for 4 h, Tirofiban produced a 2.5-fold increase in bleeding time and 97% inhibition of ADP-induced platelet aggregation.

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