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NQ301
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。
NQ301图片
CAS NO:130089-98-4
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
NQ301 是一种抗血栓剂,能够抑制胶原蛋白激发的兔血小板聚集,IC50=10 mg/mL。

产品描述

NQ301, an antithrombotic agent, inhibits collagen-challenged rabbit platelet aggregation (IC50: 10 mg/mL).

体外活性

NQ301 dose-dependently inhibits collagen (10 mg/mL, IC50: 0.60±0.02 μM), U46619 (1 mg/mL, IC50: 0.58±0.04 μM) and arachidonic acid (100 mg/mL, IC50: 0.78±0.04 μM) challenged rabbit platelet aggregation. NQ301 potently suppresses thromboxane B2 formation by platelets that are exposed to arachidonic acid in a concentration-dependent manner, but had no effect on the production of prostaglandin D2, indicating an inhibitory effect on thromboxane A2 synthase. NQ301 markedly inhibits the increase of cytosolic Ca2+ concentration and ATP secretion, and also markedly increases platelet cAMP levels in the activated platelets. The antiplatelet activity of NQ301 may be mediated by inhibition of cytosolic Ca2+ mobilization, enhancement of cAMP production and inhibition of ATP secretion in activated platelets.

激酶实验

Compounds are dissolved in DMSO (5 mg/mL) and diluted with PBS/EtOH (70:30).Kinetic analyses are carried out for TB5 and TB8. A set of Lineweaver–Burk plots are constructed in the absence and presence of various concentrations of compounds TB5 and TC8. The set consists of five graphs, each constructed by measuring MAO-B and MAO-A catalytic rates at different substrate concentrations (0.1-1 μM). The first Lineweaver–Burk plot is constructed in the absence of inhibitor, while the remaining four graphs are constructed in the presence of different concentrations of TB5 and TB8[1].

细胞实验

ished rabbit platelet suspension is challenged by addition of collagen (10 mg/mL), arachidonic acid (100 μM) or U46619 (1 μM). Concentration- response relationship is determined in the absence or presence of a range of concentrations of NQ301 (0, 0.25, 0.5, 0.75, 1 μM); aspirin-treated platelets (50 μM for 5 min) are used to prevent any possible contribution of endogenous arachidonic acid metabolites to platelet aggregation. The resulting aggregation, measured as the change in light transmission, is recorded for 5 min. The extent of platelet aggregation is expressed as % of the control[1].

Cas No.

130089-98-4

分子式

C18H12ClNO3

分子量

325.75

储存和溶解度

DMSO:29 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years