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Ticagrelor
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ticagrelor图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议
100mg电议

产品介绍
Ticagrelor (AZD6140) 是一种可逆的口服 P2Y12 受体拮抗剂,用于治疗血小板聚集。

Animal experiment:

Rats: Prasugrel (10 mg/kg, p.o.) and ticagrelor (30 mg/kg, p.o.), doses that produced similar levels of inhibition of platelet aggregation, are administered to rats 4 h before the bleeding time measurements. Fresh, washed platelets (1 × 1010 platelets/mL) are prepared from other rats and suspended in Hank's balanced salt solution. Platelets are transfused via the jugular vein to rats 1 h before the bleeding time measurements and the bleeding time is determined[3]. [2]Mice: Female BALB/c mice are inoculated subcutaneously in the fourth mammary pad with 4T1 breast cancer cells. Once a tumor is palpable, mice receive daily injections of PBS or ticagrelor (10 mg/kg). One week later, mice undergo primary tumor resection. At 28 days mice are sacrificed and lungs, femurs and tibiae harvested. Dissociated cells from lung and bone marrow are plated in medium containing 60 μM 6-thioguanine. After 14 days, culture plates are fixed with methanol and stained with 0.03% methylene blue to enumerate metastatic 4T1 colonies[2].

产品描述

Ticagrelor is a novel antagonist of the P2Y12 receptor [1].

Ticagrelor has been reported to inhibit the prothrombotic effects of ADP on the platelet by against the P2Y12 receptor. Ticagrelor has shown the complete inhibition of platelet aggregation ex vivo. In addition Ticagrelor has suggested a dose-dependent inhibition of platelet aggregation in human being. Apart from these, Ticagrelor has also demonstrated an orally, actively, reversibly binding antagonist. Unlike other inhibitors, Ticagrelor has also reported to inhibit P2Y12 receptor without metabolic transformation. Besides that, Ticagrelor is the first thienopyridine anti-platelet agent and mainly metabolized by CYP3A4 and CYP2C19 [1][2].

References:
[1] Zhou D1, Andersson TB, Grimm SW. In vitro evaluation of potential drug-drug interactions with ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, and differential kinetics. Drug Metab Dispos. 2011 Apr;39(4):703-10.
[2] Li Y1, Landqvist C, Grimm SW. Disposition and metabolism of ticagrelor, a novel P2Y12 receptor antagonist, in mice, rats, and marmosets. Drug Metab Dispos. 2011 Sep;39(9):1555-67. doi: 10.1124/dmd.111.039669. Epub 2011 Jun 13.