Aspirin-ASA-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAspirinCat. No.: HY-14654CAS No.: 50-78-2Synonyms: ASA; Acetylsalicylic Acid分式: CHO分量: 180.16作靶点: COX; Autophagy; Mitophagy作通路: Immunology/Inflammation; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 m

2、onth溶解性数据体外实验 DMSO : 100 mg/mL (555.06 mM; Need ultrasonic)H2O : 0.1 mg/mL (0.56 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration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，并请注意储备液的保存式和期限。体内实

3、验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：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 solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (

4、13.88 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (13.88 mM); Clear solutionBIOLOGICAL 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。IC50 & Target COX-1 COX-227.75 M (IC50) 1.17 mM (IC50)体外研究 Aspirin

5、and other non-steroid anti-inflammatory drugs inhibit the activity of cyclooxygenase (COX) whichleads to the formation of prostaglandins (PGs) that cause inflammation, swelling, pain and fever 2. Aspirinacetylates serine-530 of cyclooxygenase-1 (COX-1), thereby blocking thromboxane A synthesis in pl

6、ateletsand reducing platelet aggregation. This mechanism of action accounts for the effect of aspirin on preventionof coronary artery and cerebrovascular thrombosis. Aspirin is less effective in inhibiting COX-2 activity.Aspirin and salicylate inhibit COX-2 protein expression through interference wi

7、th binding of CCAAT/enhancerbinding protein beta (C/EBPbeta) to its cognate site on COX-2 promoter/enhancer 3. Aspirin inhibits theactivation of NF-B. This inhibition prevents the degradation of the NF-B inhibitor, 1B, and therefore NF-Bis retained in the cytosol. Aspirin also inhibits NF-B-dependen

8、t transcription from the lg enhancer and thehuman immunodeficiency virus (HIV) long terminal repeat (LTR) in transfected T cells 4. Aspirin inhibitsCOX-1 and COX-2 with IC50 values of 3.57 M and 29.3 M, respectively in human articular chondrocytes5.PROTOCOLCell Assay 5 Chondrocytes are isolated from

9、 articular cartilage of donors with no articular disease. Unstimulated andinterleukin 1 (IL-1) stimulated chondrocytes are used as models to study the effects of drugs on COX-1 andCOX-2. Cells are incubated with vehicle or drugs (Asprin); supernatants are removed and the level ofprostaglandin E2 (PG

10、E2) in each sample is determined by enzyme immunoassay. IC50s are calculated fromthe reduction in PGE2 content by different concentrations of the test substance by linear 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 C

11、ancer Res. 2018 Oct 1;78(19):5586-5599. Cell Death Dis. 2018 Aug 28;9(9):847.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Mitchell JA, et al. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and

12、 induciblecyclooxygenase. Proc NatlAcad 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 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. 1999Jun;26(6):1366-73.McePdfHei