水杨酸作用机制 - Medchemexpress - MCE中国

1、Product Data SheetSalicylic acidCat. No.: HY-B0167CAS No.: 69-72-7分式: CHO分量: 138.12作靶点: COX; Autophagy; Mitophagy; Endogenous Metabolite; Apoptosis作通路: Immunology/Inflammation; Autophagy; Metabolic Enzyme/Protease; Apoptosis储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (pro

2、tect from light)溶解性数据体外实验 DMSO : 100 mg/mL (724.01 mM; Need ultrasonic)H2O : 1 mg/mL (7.24 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 7.2401 mL 36.2004 mL 72.4008 mL5 mM 1.4480 mL 7.2401 mL 14.4802 mL10 mM 0.7240 mL 3.6200 mL 7.2401 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

3、，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 (protect from light)。-80C 储存时，请在 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

4、剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (18.10 mM); Clear solution此案可获得 2.5 mg/mL (18.10 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)Solubi

5、lity: 2.5 mg/mL (18.10 mM); Clear solution此案可获得 2.5 mg/mL (18.10 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Page 1 of 2 www.MedChemE均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (18.10 mM); Clear solution此案可获得 2.5 mg/mL (18.10 mM，饱和度未知) 的澄 溶

6、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。BIOLOGICAL ACTIVITY物活性 Salicylic acid 抑制 COX-2 活性，抑制作与转录因 (NF-B) 激活关。IC & Target COX-2 Human Endogenous Autophagy MitophagyMetabolite体外研究 Salicylic acid is an effective inhibitor of COX-2 activity at concentrations far b

7、elow those required to inhibit NF-B (20mg/mL) activation. Salicylic acid inhibits prostaglandin E2 release when add together with interleukin 1 for 24 hr withan IC50 value of 5 g/mL, an effect that is independent of NF-B activation or COX-2 transcription or translation.Salicylic acid acutely (30 min

8、) also causes a concentration-dependent inhibition of COX-2 activity measured in thepresence of 0, 1, or 10 M exogenous arachidonic acid. In contrast, when exogenous arachidonic acid is increased to30 M, Salicylic acid is a very weak inhibitor of COX-2 activity with an IC50 of 100 g/mL. When added t

9、ogether withIL-1 for 24 hr, Salicylic acid causes a concentration-dependent inhibition of PGE2 release with an apparent IC50 valueof approximately 5 g/mL. The ability of Salicylic acid to directly inhibit COX-2 activity in A549 cells is tested after a30-min exposure period, followed by the addition

10、of different concentrations of exogenous arachidonic acid (1, 10,and 30 M). Salicylic acid causes a concentration-dependent inhibition of COX-2 activity in the absence of addedarachidonic acid or in the presence of 1 or 10 M exogenous substrate with an apparent IC50 value of approximately5 g/mL. How

11、ever, when the same experiments are performed using 30 M arachidonic acid, Salicylic acid is anineffective inhibitor of COX-2 activity, with an apparent IC50 value of more than 100 g/mL, and achieves a maximalinhibition of less than 50%1.体内研究 In C57Bl/6 DIO mice, Salicylic acid decreases both fastin

12、g and postprandial plasma glucose levels. Furthermore, thereis a trend to reduce plasma triglyceride levels after Salicylic acid treatment in C57Bl/6 DIO mice (P=0.059). Salicylic acid significantly reduces 11-HSD1 mRNA in omental adipose tissue in C57Bl/6 DIO mice, with a similar trend inmesenteric

13、 adipose (P=0.057). In mesenteric adipose of C57Bl/6 DIO mice, Salicylic acid also reduces 11-HSD1enzyme activity2.PROTOCOLKinase Assay 1 Human purified COX-2 are and the cofactors Glutathione (5 mM), Adrenaline (5 mM), and Hematin (1 M) aredissolved in 50 mM Tris buffer (pH 7.5). Hematin is first d

14、issolved in a concentrated stock of 100 mM in 1 M NaOHbefore being further diluted in Tris buffer. Enzyme reactions are carried out in individual wells of 96-well plates with afinal reaction volume of 200 L. Different concentrations of Salicylic acid are added to the plate, followed by theaddition o

15、f 10 units of enzyme (180 L). The plates are incubated at 37 for 30 min before Arachidonic acid (10 nM to30 M) is added for a further 15 min. The reaction is stopped by heating the plate to 100C for 5 min. The 96-wellplate is then centrifuged at 10,000 g for 10 min, and appropriated samples are remo

16、ved and added into theradioimmunoassay1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 To assess the direct effect of Salicylic acid on COX-2 activity after induction has occurred, A549 cells are first treatedPage 2 of 3 www.MedChemEwith I

17、L-1 for 24 hr, and the culture medium is replaced with DMEM containing different concentrations of Salicylicacid(10, 100 and 1000 g/mL). Cells are incubated at 37C for 30 min. Arachidonic acid (1-30 M) is then added for15 min, and the medium is removed for the measurement of PGE21.MCE has not indepe

18、ndently confirmed the accuracy of these methods. They are for reference only.Animal Mice2Administration 2 Adult male C57Bl/6 mice are at age 12 weeks. Diet-induced obese C57Bl/6 mice (C57Bl/6 DIO) are given 10 weeksof high-fat diet (58% fat, 12% sucrose) before treatment. Salicylic acid (120 mg/kg/d

19、ay) is administered from 1 weekafter arriving (C57Bl/6 Lean), after 10 weeks of high-fat feeding (C57Bl/6 DIO), or after achieving target weight(HSD1KO-DIO) for 4 weeks to groups of n=8 via osmotic minipumps implant subcutaneously between the scapulae.MCE has not independently confirmed the accuracy of these methods. They are for referen