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• 產(chǎn)品描述： NQ301 is an antithrombotic agent; inhibits collagen-challenged rabbit platelet aggregation with an IC50 of 10 mg/mL.

• 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.

• 溶解性： Soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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

• 注意：部分產(chǎn)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。

輸入產(chǎn)品批號：

本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *