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NQ301

Catalog No. T3757   CAS 130089-98-4

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

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NQ301 Chemical Structure
NQ301, CAS 130089-98-4
Pack Size Availability Price/USD Quantity
5 mg In stock $ 53.00
10 mg In stock $ 77.00
25 mg In stock $ 126.00
50 mg In stock $ 207.00
100 mg In stock $ 369.00
500 mg In stock $ 885.00
1 mL * 10 mM (in DMSO) In stock $ 57.00
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Purity: 99.81%
Purity: 99.76%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description NQ301, an antithrombotic agent, inhibits collagen-challenged rabbit platelet aggregation (IC50: 10 mg/mL).
Targets&IC50 Platelet aggregation (rabbit, collagen-challenged):10 mg/mL
In vitro 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.
Kinase Assay 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].
Cell Research 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].
Molecular Weight 325.75
Formula C18H12ClNO3
CAS No. 130089-98-4

Storage

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

Solubility Information

DMSO: 29 mg/mL

TargetMolReferences and Literature

1. Jin YR, et al. An antithrombotic agent, NQ301, inhibits thromboxane A2 receptor and synthase activity in rabbit platelets. Basic Clin Pharmacol Toxicol. 2005 Sep;97(3):162-7. 2. Zhang YH, et al. Antiplatelet effect of 2-chloro-3-(4-acetophenyl)-amino-1,4-naphthoquinone (NQ301): a possible mechanism through inhibition of intracellular Ca2+ mobilization. Biol Pharm Bull. 2001 Jun;24(6):618-22.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Coagulation and Anticoagulation Compound Library Anti-Metabolism Disease Compound Library Endocrinology-Hormone Compound Library Preclinical Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cardiovascular Disease Compound Library Immunology/Inflammation Compound Library Protease Inhibitor Library

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Keywords

NQ301 130089-98-4 Others Proteases/Proteasome Thrombin Platelet aggregation inhibit Inhibitor NQ 301 NQ-301 inhibitor

 

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