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產品描述： NQ301 is an antithrombotic agent; inhibits collagen-challenged rabbit platelet aggregation with an IC50 of 10 mg/mL. |
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靶點：
IC50: 0.60±0.02 μM (collagen-challenged rabbit platelet aggregation), 0.58±0.04 μM (U46619-challenged rabbit platelet aggregation), 0.78±0.04 μM (arachidonic acid-challenged rabbit platelet aggregation);Thrombin;?Plateletaggregation |
體外研究：
NQ301 concentration-dependently inhibits collagen (10 mg/mL)-, U46619 (1 mg/mL)- and arachidonic acid (100 mg/mL)-challenged rabbit platelet aggregation, with IC50 values of 0.60±0.02, 0.58±0.04 and 0.78±0.04 μM, respectively. 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 has a potential to inhibit thromboxane A2 synthase activity with thromboxane A2/prostaglandin H2 receptor blockade, and modulate arachidonic acid liberation as well as 12-hydroxy-5,8,10,14-eicosatetraenoic acid formation in platelets. NQ301 inhibits platelet aggregation by suppression of the intracellular pathway, rather than by direct inhibition of fibrinogen-GPIIb/IIIa complex binding. NQ301 significantly inhibits the increase of cytosolic Ca2+ concentration and ATP secretion, and also significantly 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. |
參考文獻：
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. |
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溶解性：
Soluble in DMSO |
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保存條件：
-20℃ |
配置溶液濃度參考：
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1mg |
5mg |
10mg |
| 1 mM |
3.07 ml |
15.349 ml |
30.699 ml |
| 5 mM |
0.614 ml |
3.07 ml |
6.14 ml |
| 10 mM |
0.307 ml |
1.535 ml |
3.07 ml |
| 50 mM |
0.061 ml |
0.307 ml |
0.614 ml |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
北京