Ticagrelor

A reversible purinergic P2Y12 receptor antagonist

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
10mg

￥425.00

340.00

- +
50mg

￥612.00

490.00

- +
100mg

￥950.00

760.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajci14906
CAS: 274693-27-5
别名: 替卡格雷; AZD6140; AR-C 126532XX
分子式: C23H28F2N6O4S
分子量: 522.57
纯度: >98%
溶解度: ≥ 26.15mg/mL in DMSO
储存: Store at -20°C, protect from light, stored under nitrogen
库存: 现货

Background

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].

参考文献:
[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.

Protocol

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].

参考文献:

[1]. Aungraheeta R, et al. Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor. Blood. 2016 Dec 8;128(23):2717-2728.
[2]. Gebremeskel S, et al. The reversible P2Y12 inhibitor ticagrelor inhibits metastasis and improves survival in mouse models of cancer. Int J Cancer. 2015 Jan 1;136(1):234-40.
[3]. Sugidachi A, et al. A comparison of the pharmacological profiles of prasugrel and ticagrelor assessed by platelet aggregation, thrombus formation and haemostasis in rats. Br J Pharmacol. 2013 May;169(1):82-9.