阿司匹林作用机制 - Medchemexpress - MCE中国

1、Product Data SheetAspirinCat. No.: HY-14654CAS No.: 50-78-2分式: CHO分量: 180.16作靶点: COX; Autophagy; Mitophagy; Virus Protease作通路: Immunology/Inflammation; Autophagy; Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (555.06 mM; Need ultrasoni

2、c)H2O : 0.1 mg/mL (0.56 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 5.5506 mL 27.7531 mL 55.5062 mL5 mM 1.1101 mL 5.5506 mL 11.1012 mL10 mM 0.5551 mL 2.7753 mL 5.5506 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在

3、 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (13.88 mM); Clear sol

4、ution此案可获得 2.5 mg/mL (13.88 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (13.88 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (13.88

5、 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (13.88 mM); Clear solution此案可获得 2.5 mg/mL (13.88 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGIC

6、AL ACTIVITY物活性 Aspirin选择性和不可逆的 COX-1 和 COX-2 抑制剂，IC50 分别为5，210 g/mL。IC & Target COX-1 COX-227.75 M (IC50) 1.17 mM (IC50)体外研究 Aspirin and other non-steroid anti-inflammatory drugs inhibit the activity of cyclooxygenase (COX) which leads to theformation of prostaglandins (PGs) that cause inflammation,

7、 swelling, pain and fever2. Aspirin acetylates serine-530 ofcyclooxygenase-1 (COX-1), thereby blocking thromboxane A synthesis in platelets and reducing platelet aggregation.This mechanism of action accounts for the effect of aspirin on prevention of coronary artery and cerebrovascularthrombosis. As

8、pirin is less effective in inhibiting COX-2 activity. Aspirin and salicylate inhibit COX-2 protein expressionthrough interference with binding of CCAAT/enhancer binding protein beta (C/EBPbeta) to its cognate site on COX-2promoter/enhancer3. Aspirin inhibits the activation of NF-B. This inhibition p

9、revents the degradation of the NF-Binhibitor, 1B, and therefore NF-B is retained in the cytosol. Aspirin also inhibits NF-B-dependent transcription fromthe lg enhancer and the human immunodeficiency virus (HIV) long terminal repeat (LTR) in transfected T cells4.Aspirin inhibits COX-1 and COX-2 with

10、IC50 values of 3.57 M and 29.3 M, respectively in human articularchondrocytes5.PROTOCOLCell Assay 5 Chondrocytes are isolated from articular cartilage of donors with no articular disease. Unstimulated and interleukin 1(IL-1) stimulated chondrocytes are used as models to study the effects of drugs on

11、 COX-1 and COX-2. Cells areincubated with vehicle or drugs (Asprin); supernatants are removed and the level of prostaglandin E2 (PGE2) in eachsample is determined by enzyme immunoassay. IC50s are calculated from the reduction in PGE2 content by differentconcentrations of the test substance by linear

12、 regression analysis5.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cancer Res. 2018 Oct 1;78(19):5586-5599. Cell Death Dis. 2018 Aug 28;9(9):847.See more customer validations on HYPERLINK www.MedChemE www.MedChemEPage 2 of 3 www.MedChemER

13、EFERENCES1. Mitchell JA, et al. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and induciblecyclooxygenase. Proc Natl Acad Sci U S A.1993 Dec 15;90(24):11693-7.2. Vane JR, et al. The mechanism of action of aspirin. Thromb Res. 2003 Jun 15;110(5-6):255-8.3. Wu KK, et

14、 al. Aspirin and other cyclooxygenase inhibitors: new therapeutic insights. Semin Vasc Med. 2003 May;3(2):107-12.4. Kopp E, et al. Inhibition of NF-kappa B by sodium salicylate and aspirin. Science. 1994 Aug 12;265(5174):956-9.5. Blanco FJ, et al. Effect of antiinflammatory drugs on COX-1 and COX-2 activity in human articular chondrocytes. J Rheumatol. 1999 Jun;26(6):1366-73.McePdfHe