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| 50g |
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Purity: ≥98%
Sodium salicylate (Magsalyl; Kerasalicyl; Kerosal), the sodium salt of salicylic acid and a metabolite of acetylsalicylic acid, is an inhibitor of NF-kB with potential anti-inflammatory activity. It has been used as a nonsteroidal anti-inflammatory drug (NSAID). It works by permanently acetylating COX I/II (cyclooxygenases I and II), which prevents the production of prostaglandins, which is a key factor in inflammation and pain.
| Targets |
COX-2; Microbial Metabolite; Autophagy; S6K
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| ln Vitro |
At concentrations much lower than those necessary to prevent the activation of NF-κB (20 mg/mL), sodium salicylate effectively inhibits COX-2 activity. When combined with interleukin 1β for 24 hours, sodium salicylate inhibits prostaglandin E2 release with an IC50 value of 5 μg/mL, an effect that is not influenced by NF-κB activation, COX-2 transcription, or COX-2 translation. Additionally, sodium salicylate acutely (30 min) inhibits COX-2 activity as measured in the presence of 0, 1, or 10 μM exogenous arachidonic acid in a concentration-dependent manner. In contrast, sodium salicylate is a very weak inhibitor of COX-2 activity with an IC50 of >100 μg/mL when exogenous arachidonic acid is increased to 30 μM. With an apparent IC50 value of about 5 μg/mL when combined with IL-1 for 24 hours, sodium salicylate inhibits PGE2 release in a concentration-dependent manner. After a 30-min exposure period, different concentrations of exogenous arachidonic acid (1, 10, and 30 μM) are added, and then the ability of sodium salicylate to directly inhibit COX-2 activity in A549 cells is tested. In the absence of additional arachidonic acid or in the presence of 1 or 10 μM exogenous substrate, sodium salicylate inhibits COX-2 activity in a concentration-dependent manner, with an apparent IC50 value of roughly 5 μg/mL. With an apparent IC50 value of more than 100 g/mL and a maximal inhibition of less than 50%, sodium salicylate is an ineffective inhibitor of COX-2 activity when the same experiments are carried out using 30 μM arachidonic acid[1].
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| ln Vivo |
Salicylate lowers plasma glucose levels in C57Bl/6 DIO mice during fasting and after meals. Additionally, after Salicylate treatment in C57Bl/6 DIO mice, there is a tendency to decrease plasma triglyceride levels (P=0.059). Salicylate significantly lowers 11β-HSD1 mRNA in the omental adipose tissue of C57Bl/6 DIO mice, with a trend toward the same result in the mesenteric adipose (P=0.057). Salicylate also lowers 11β-HSD1 enzyme activity in the mesenteric adipose of C57Bl/6 DIO mice[2].
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| Enzyme Assay |
The cofactors Glutathione (5 mM), Adrenaline (5 mM), and Hematin (1 M) are dissolved in 50 mM Tris buffer (pH 7.5), along with human purified COX-2. Prior to further diluting in Tris buffer, hematin is first dissolved in a concentrated stock of 100 mM in 1 M NaOH. 96-well plates with individual wells are used to conduct enzyme reactions, with a final reaction volume of 200 μL. The plate is first filled with various sodium salicylate concentrations, then 10 enzyme units (180 μL) are added. Arachidonic acid (10 nM to 30 μM) is then added to the plates and incubated at 37 ° for an additional 15 min. The reaction is stopped by heating the plate to 100°C for five minutes. The 96-well plate is then centrifuged at 10,000 g for 10 min, after which the appropriate samples are taken out and added to the radioimmunoassay[1].
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| Cell Assay |
A549 cells are first treated with IL-1β for 24 hours, and the culture medium is replaced with DMEM containing different concentrations of sodium salicylate (10, 100, and 1000 μg/mL) in order to assess the direct effect of sodium salicylate on COX-2 activity after induction. For 30 minutes, cells are incubated at 37°C. Following a 15-minute addition of arachide acid (1–30 μM), the medium is removed to measure PGE2[1].
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| Animal Protocol |
Mice: Male C57Bl/6 adult mice are 12 weeks old. Prior to treatment, 10 weeks of a high-fat diet (58% fat, 12% sucrose) are given to C57Bl/6 mice that have developed diet-induced obesity (C57Bl/6 DIO). To groups of n=8, osmotic minipumps implanted subcutaneously between the scapulae are used to administer sodium salicylate (120 mg/kg/day) or distilled water (vehicle) starting one week after arrival (C57Bl/6 Lean), after ten weeks of high-fat feeding (C57Bl/6 DIO), or after reaching the target weight (HSD1KO-DIO) for four weeks.
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| References |
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| Additional Infomation |
Sodium salicylate is an organic molecular entity.
Sodium Salicylate is the sodium salt of salicylic acid. As a nonsteroidal anti-inflammatory drug (NSAID), sodium salicylate irreversibly acetylates cyclooxygenases I and II, thereby inhibiting prostaglandin synthesis and associated inflammation and pain. This agent may also activate mitogen-activated protein kinase (p38MAPK), thereby inducing apoptosis in cancer cells. (NCI04) A non-steroidal anti-inflammatory agent that is less effective than equal doses of ASPIRIN in relieving pain and reducing fever. However, individuals who are hypersensitive to ASPIRIN may tolerate sodium salicylate. In general, this salicylate produces the same adverse reactions as ASPIRIN, but there is less occult gastrointestinal bleeding. (From AMA Drug Evaluations Annual, 1992, p120) See also: Salicylic Acid (has active moiety); Methenamine; Sodium Salicylate (component of) ... View More ... |
| Molecular Formula |
C7H6O3.NA
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| Molecular Weight |
161.11
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| Exact Mass |
160.013
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| Elemental Analysis |
C, 52.51; H, 3.15; Na, 14.36; O, 29.98
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| CAS # |
54-21-7
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| Related CAS # |
Salicylic acid;69-72-7
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| PubChem CID |
16760658
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| Appearance |
White to off-white solid powder
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| Boiling Point |
336.3ºC at 760mmHg
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| Melting Point |
>300 °C(lit.)
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| Flash Point |
144.5ºC
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| Index of Refraction |
1.435
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
11
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| Complexity |
138
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Na+].O([H])C1=C([H])C([H])=C([H])C([H])=C1C(=O)[O-]
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| InChi Key |
ABBQHOQBGMUPJH-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C7H6O3.Na/c8-6-4-2-1-3-5(6)7(9)10;/h1-4,8H,(H,9,10);/q;+1/p-1
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| Chemical Name |
sodium;2-hydroxybenzoate
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| Synonyms |
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (15.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (15.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (15.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 110 mg/mL (687.07 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.2069 mL | 31.0347 mL | 62.0694 mL | |
| 5 mM | 1.2414 mL | 6.2069 mL | 12.4139 mL | |
| 10 mM | 0.6207 mL | 3.1035 mL | 6.2069 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05069740 | Recruiting | Drug: Salsalate Pill Drug: Placebo |
Endometriosis | Penn State University | January 1, 2022 | Early Phase 1 |
| NCT03229408 | Recruiting | Drug: Salsalate Other: Placebo |
Polycystic Ovary Syndrome | University of Illinois at Chicago |
December 5, 2018 | Phase 2 |
| NCT01480297 | Completed | Drug: Salsalate | Type 1 Diabetes Peripheral Neuropathy |
University of Michigan | November 2011 | Phase 2 |
| NCT01182727 | Completed | Drug: salsalate | Schizophrenia Insulin Resistance |
University of Maryland, Baltimore |
August 2010 | Not Applicable |
| NCT01046682 | Completed | Drug: Salsalate | HIV Inflammation |
University Hospitals Cleveland Medical Center |
January 2009 | Phase 2 |
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