Salicylic-acid-2-Hydroxybenzoic-acid-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESalicylic acidCat. No.: HY-B0167CAS No.: 69-72-7Synonyms: 2-Hydroxybenzoic acid分式: CHO分量: 138.12作靶點: COX; Autophagy; Mitophagy作通路: Immunology/Inflammation; Autophagy儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C,

2、 1 month (protect fromlight)溶解性數(shù)據(jù)體外實驗 DMSO : 700 mg/mL (5068.06 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和

3、期限。BIOLOGICAL ACTIVITY物活性 Salicylic acid 抑制 COX-2 活性，抑制作與轉(zhuǎn)錄因 (NF-B) 激活關(guān)。IC50 & Target COX-2 Autophagy Mitophagy體外研究Salicylic acid is an effective inhibitor of COX-2 activity at concentrations far below those required to inhibitNF-B (20 mg/mL) activation. Salicylic acid inhibits prostaglandin E2 rele

4、ase when add together with1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEinterleukin 1 for 24 hr with an IC50 value of 5 g/mL, an effect that is independent of NF-B activation orCOX-2 transcription or translation. Salicylic acid acutely (30 min) also causes a concentration-dependentinhibition of C

5、OX-2 activity measured in the presence of 0, 1, or 10 M exogenous arachidonic acid. Incontrast, when exogenous arachidonic acid is increased to 30 M, Salicylic acid is a very weak inhibitor ofCOX-2 activity with an IC50 of 100 g/mL. When added together with IL-1 for 24 hr, Salicylic acid causes acon

6、centration-dependent inhibition of PGE2 release with an apparent IC50 value of approximately 5 g/mL.The ability of Salicylic acid to directly inhibit COX-2 activity in A549 cells is tested after a 30-min exposureperiod, followed by the addition of different concentrations of exogenous arachidonic ac

7、id (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 ofapproximately 5 g/mL. However, when the same experiments are performed using 30

8、M arachidonic acid,Salicylic acid is an ineffective inhibitor of COX-2 activity, with an apparent IC50 value of more than 100 g/mL, and achieves a maximal inhibition of less than 50% 1.體內(nèi)研究 In C57Bl/6 DIO mice, Salicylic acid decreases both fasting and postprandial plasma glucose levels.Furthermore,

9、 there is a trend to reduce plasma triglyceride levels after Salicylic acid treatment in C57Bl/6DIO mice (P=0.059). Salicylic acid significantly reduces 11-HSD1 mRNA in omental adipose tissue inC57Bl/6 DIO mice, with a similar trend in mesenteric adipose (P=0.057). In mesenteric adipose of C57Bl/6DI

10、O mice, Salicylic acid also reduces 11-HSD1 enzyme activity 2.PROTOCOLKinase Assay 1 Human purified COX-2 are and the cofactors Glutathione (5 mM), Adrenaline (5 mM), and Hematin (1 M)are dissolved in 50 mM Tris buffer (pH 7.5). Hematin is first dissolved in a concentrated stock of 100 mM in 1M NaOH

11、 before being further diluted in Tris buffer. Enzyme reactions are carried out in individual wells of 96-well plates with a final reaction volume of 200 L. Different concentrations of Salicylic acid are added to theplate, followed by the addition of 10 units of enzyme (180 L). The plates are incubat

12、ed at 37 for 30 minbefore Arachidonic acid (10 nM to 30 M) is added for a further 15 min. The reaction is stopped by heatingthe plate to 100C for 5 min. The 96-well plate is then centrifuged at 10,000 g for 10 min, and appropriatedsamples are removed and added into the radioimmunoassay 1.MCE has not

13、 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 firsttreated with IL-1 for 24 hr, and the culture medium is replaced with DMEM containing diff

14、erentconcentrations of Salicylic acid(10, 100 and 1000 g/mL). Cells are incubated at 37C for 30 min.Arachidonic acid (1-30 M) is then added for 15 min, and the medium is removed for the measurement ofPGE2 1.MCE has not independently confirmed the accuracy of these methods. They are for reference onl

15、y.Animal Mice 2Administration 2 Adult male C57Bl/6 mice are at age 12 weeks. Diet-induced obese C57Bl/6 mice (C57Bl/6 DIO) are given 10weeks of high-fat diet (58% fat, 12% sucrose) before treatment. Salicylic acid (120 mg/kg/day) isadministered from 1 week after arriving (C57Bl/6 Lean), after 10 wee

16、ks of high-fat feeding (C57Bl/6 DIO), or2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEafter achieving target weight (HSD1KO-DIO) for 4 weeks to groups of n=8 via osmotic minipumps implantsubcutaneously between the scapulae.MCE has not independently confirmed the accuracy of these methods. They ar

17、e for reference only.REFERENCES1. Mitchell JA, et al. Sodium salicylate inhibits cyclo-oxygenase-2 activity independently of transcription factor (nuclear factor kappaB)activation: role of arachidonic acid. Mol Pharmacol. 1997 Jun;51(6):907-12.2. Nixon M, et al. Salicylate downregulates 11-HSD1 expression in adipose tissue in obese mice and in humans, medi