化合物NQ301 T3757

Product Introduction
Bioactivity


英文名: NQ301

描述: 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。

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].

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].

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 29 mg/mL


关键字: inhibit | Inhibitor | NQ 301 | NQ301 | NQ-301 | Thrombin

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相关库: Coagulation and Anticoagulation Compound Library | Anti-Metabolism Disease Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Endocrinology-Hormone Compound Library | Protease Inhibitor Library | Preclinical Compound Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compound Library

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