| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
COX-1
COX-1/2
|
|---|---|
| ln Vitro |
In human articular chondrocytes, lithium aspirin inhibits COX-1 and COX-2, with IC50 values of 3.57 μM and 29.3 μM, respectively [2]. By acetylating serine 530 of COX-1, lithium aspirin inhibits the production of thromboxane A in platelets and decreases platelet aggregation [3]. By preventing CCAAT/enhancer binding protein beta (C/EBPbeta) from attaching to its appropriate location on the COX-2 promoter/enhancer, lithium aspirin suppresses the expression of the COX-2 protein [3]. In transfected T cells, lithium aspirin suppresses the transcription of the lgκ enhancer and the HIV long terminal repeat (LTR) in an NF-κB-dependent manner [4]. By triggering caspases, p38 MAP kinase, mitochondrial cytochrome c release, and the ceramide pathway, lithium aspirin causes apoptosis [6].
|
| ln Vivo |
In adult male rats with yeast fever, lithium aspirin (5–150 mg/kg, oral, once) exhibits strong antipyretic effects [7].
|
| Enzyme Assay |
The transcription factor nuclear factor-kappa B (NF-kappa B) is critical for the inducible expression of multiple cellular and viral genes involved in inflammation and infection including interleukin-1 (IL-1), IL-6, and adhesion molecules. The anti-inflammatory drugs sodium salicylate and aspirin inhibited the activation of NF-kappa B, which further explains the mechanism of action of these drugs. This inhibition prevented the degradation of the NF-kappa B inhibitor, I kappa B, and therefore NF-kappa B was retained in the cytosol. Sodium salicylate and aspirin also inhibited NF-kappa B-dependent transcription from the Ig kappa enhancer and the human immunodeficiency virus (HIV) long terminal repeat (LTR) in transfected T cells.[4]
Aspirin inhibits platelet function by permanently acetylating the cyclooxygenase that forms prostaglandins. We determined the sensitivity of platelets to aspirin in normal subjects by measuring [3H-acetyl]aspirin-susceptible cyclooxygenase in washed platelets obtained at various times after aspirin ingestion. A single 325-mg aspirin dose inactivated 89% of platelet cyclooxygenase. The inhibition persisted for 2 days suggesting that oral aspirin also inactivated megakaryocyte cyclooxygenase. Thereafter, active enzyme returned with a time-course reflecting platelet turnover (life-span 8.2+/-2 days). Single doses of 20-650 mg aspirin resulted in 34- greater than 95% inhibition after 24 h. Daily doses of 20-325 mg aspirin for brief periods produced 61- greater than 95% inactivation when measured 24 h after cessation of the drug. Platelet cyclooxygenase is more sensitive to inactivation by aspirin than enzyme in sheep seminal vesicles.[4] |
| Animal Protocol |
Animal/Disease Models: Male albino Charles River rats (200-250 g, 8 rats/group, use 20 ml/kg 20% beer yeast aqueous suspension to induce fever, subcutaneously (sc) (sc) injected on the back below the nape of the neck) [7]
Doses: 5, 25, 50, 100 and 150 mg/kg Doses: po (po (oral gavage)) once Experimental Results: The 150 mg/kg dose produced a statistically significant decrease of 0.23°C 15 minutes after dosing. The antipyretic effect gradually increased until reaching a peak value of 1.96°C 120 minutes after administration. The ED50 of aspirin is 10.3 mg/kg, with a confidence limit of 1.8-23.0 mg/kg. The antipyretic response of aspirin depends on the dose of the compound administered. |
| References | |
| Additional Infomation |
Evidence from a wide range of sources suggests that individuals taking aspirin and related non-steroidal anti-inflammatory drugs have reduced risk of large bowel cancer. Work in animals supports cancer reduction with aspirin, but no long-term randomised clinical trials exist in human beings, and randomisation would be ethically unacceptable because vascular protection would have to be denied to a proportion of the participants. However, opportunistic trials of aspirin, designed to test vascular protection, provide some evidence of a reduction in cancer, but only after at least 10 years. We summarise evidence for the potential benefit of aspirin and natural salicylates in cancer prevention. Possible mechanisms of action and directions for further work are discussed, and implications for clinical practice are considered.[6]
|
| Molecular Formula |
C9H7LIO4
|
|---|---|
| Molecular Weight |
186.09
|
| Exact Mass |
186.05
|
| Elemental Analysis |
C, 58.09; H, 3.79; Li, 3.73; O, 34.39
|
| CAS # |
552-98-7
|
| Related CAS # |
Aspirin;50-78-2
|
| PubChem CID |
23680279
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
321.4ºC at 760mmHg
|
| Flash Point |
131.2ºC
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
14
|
| Complexity |
217
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[Li+].CC(=O)OC1=CC=CC=C1C(=O)[O-]
|
| InChi Key |
FGLLQDSAOUJRST-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C9H8O4.Li/c1-6(10)13-8-5-3-2-4-7(8)9(11)12;/h2-5H,1H3,(H,11,12);/q;+1/p-1
|
| Chemical Name |
lithium;2-acetyloxybenzoate
|
| Synonyms |
Lithium O-acetylsalicylate; 552-98-7; lithium 2-acetoxybenzoate; Aspirin (lithium); Acetylsalicylic acid, lithium salt; lithium;2-acetyloxybenzoate; 89R59534MK; Lithium acetylsalicylate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.3737 mL | 26.8687 mL | 53.7374 mL | |
| 5 mM | 1.0747 mL | 5.3737 mL | 10.7475 mL | |
| 10 mM | 0.5374 mL | 2.6869 mL | 5.3737 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.
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