NQ301 - Thrombin - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENQ301Cat. No.: HY-101054CAS No.: 130089-98-4分式: CHClNO分量: 325.75作靶點(diǎn): Thrombin作通路: Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 29 mg/mL (89.03 mM)* means soluble

2、, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.0698 mL 15.3492 mL 30.6984 mL5 mM 0.6140 mL 3.0698 mL 6.1397 mL10 mM 0.3070 mL 1.5349 mL 3.0698 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 NQ301種抗栓劑; 可抑制膠原蛋激發(fā)的兔板聚集，IC50值為10 mg/mL。IC50 & Target IC5

3、0: 0.600.02 M (collagen-challenged rabbit platelet aggregation), 0.580.04 M (U46619-challengedrabbit platelet aggregation), 0.780.04 M (arachidonic acid-challenged rabbit platelet aggregation) 1體外研究NQ301 concentration-dependently inhibits collagen (10 mg/mL)-, U46619 (1 mg/mL)- and arachidonic acid1

4、/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE(100 mg/mL)-challenged rabbit platelet aggregation, with IC50 values of 0.600.02, 0.580.04 and 0.780.04M, respectively. NQ301 potently suppresses thromboxane B2 formation by platelets that are exposed toarachidonic acid in a concentration-dependent man

5、ner, but had no effect on the production of prostaglandinD2, indicating an inhibitory effect on thromboxane A2 synthase. NQ301 has a potential to inhibitthromboxane A2 synthase activity with thromboxane A2/prostaglandin H2 receptor blockade, and modulatearachidonic acid liberation as well as 12-hydr

6、oxy-5,8,10,14-eicosatetraenoic acid formation in platelets 1.NQ301 inhibits platelet aggregation by suppression of the intracellular pathway, rather than by directinhibition of fibrinogen-GPIIb/IIIa complex binding. NQ301 significantly inhibits the increase of cytosolic Ca2+concentration and ATP sec

7、retion, and also significantly increases platelet cAMP levels in the activatedplatelets. 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 2.PROTOCOLCell Assay 1 ished

8、rabbit platelet suspension is challenged by addition of collagen (10 mg/mL), arachidonic acid (100 M)or U46619 (1 M). Concentration- response relationship is determined in the absence or presence of a rangeof concentrations of NQ301 (0, 0.25, 0.5, 0.75, 1 M); aspirin-treated platelets (50 M for 5 mi

9、n) are used toprevent any possible contribution of endogenous arachidonic acid metabolites to platelet aggregation. Theresulting aggregation, measured as the change in light transmission, is recorded for 5 min. The extent ofplatelet aggregation is expressed as % of the control 1.MCE has not independ

10、ently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Jin YR, et al. An antithrombotic agent, NQ301, inhibits thromboxane A2 receptor and synthase activity in rabbit platelets. Basic ClinPharmacol 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 throughinhibition of intracellular Ca2+ mobilization. Biol Pharm Bull. 2001 Jun;24(6):618-22.McePdfHeightCaution: Product has not been f