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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Ibuprofen Lysine (Arflamin, Ibuprofen lysinate, NeoProfen, Saren), the pyridyl ester of ibuprofen, is an anti-inflammatory drug that belongs to the non-steroidal anti-inflammatory drug (NSAIDs) class. The MOA (mechanism of action) of Ibuprofen Lysine is to act as a non-selective COX inhibitor with an IC50 of 0.33 mM, and also has an antiplatelet effect, though Ibuprofen Lysine is relatively mild and short-lived when compared with that of aspirin or other agents.
| ln Vitro |
L-lysine (ibuprofen) (24 h) suppresses the activity of COX-1 and COX-2, with IC50 values of 13 μM and 370 μM, respectively[1]. Ibuprofen (500 μM, 48 h) L-lysine causes apoptosis in AGS cells (adenocarcinoma stomach cell line) and suppresses angiogenesis and cell proliferation[2]. In AGS cells, ibuprofen (500 μM, 48 h) L-lysine upregulates wild type P53 and Bax gene RNA levels while downregulating transcription of Akt, VEGF-A, PCNA, Bcl2, OCT3/4, and CD44 genes[2]. In both primary CF nasal epithelial cells and cystic fibrosis (CF) cell models, ibuprofen (500 μM, 24 hours) L-lysine stimulates microtubule elongation to the cell periphery and restores microtubule-dependent intracellular cholesterol transport[3]. Through photosensitization, ibuprofen (500 μM, 24 h) L-lysine amplifies UV-induced cell death in MCF-7 and MDA-MB-231 cells[4].
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| ln Vivo |
In a model of postpartum breast cancer, ibuprofen (300 mg/kg; po; daily, for 14 days) and L-lysine diminish overall tumor development and improve anti-tumor immune features without causing negative autoimmune reactions[5]. In a rat model of chronic Oxaliplatin-induced peripheral neuropathy, L-lysine lowers the incidence of neuropathy, as does ibuprofen (60 mg/kg; ih; every other day for 15 days)[6]. L-lysine reduces muscle growth (average muscle fiber cross-sectional area) without altering the control of supraspinatus tendon adaptations to exercise, when combined with ibuprofen (20 mg/kg; po; every 12 hours, 5 doses total)[7]. In a rat model of chronic lung infection, ibuprofen (35 mg/kg; po; twice daily) and L-lysine reduce the inflammatory response to pseudomonas aeruginosa[8].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: AGS cells Tested Concentrations: 100-1000 μM Incubation Duration: 24 h, 48 h Experimental Results: Inhibited AGS cell viability with IC50 values of 630 μM (trypan blue staining, 24 h), 456 μM (neutral red assay, 24 h), 549 μM (trypan blue staining, 48 h) and 408 μM (neutral red assay, 48 h). |
| Animal Protocol |
Animal/Disease Models: Syngeneic (D2A1) orthotopic Balb/c mouse model of PPBC (postpartum)[5]
Doses: 300 mg/kg, daily for 14 days Route of Administration: Fed in animal feedings (added to pulverized standard chow and mixed dry, then mixed with water, made into chow pellets and dried thoroughly) Experimental Results: Suppresed tumor growth, decreased presence of immature monocytes and increased numbers of T cells. Enhanced Th1 associated cytokines as well as promoted tumor border accumulation of T cells. Animal/Disease Models: Oxaliplatin‑induced peripheral neuropathy[6] Doses: 60 mg/kg, every second day for 15 days Route of Administration: subcutaneous (sc) injection Experimental Results: Lowered sensory nerve conduction velocity (SNCV). |
| References |
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| Additional Infomation |
See also: Ibuprofen (has active moiety).
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| Molecular Formula |
C19H32N2O4
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| Molecular Weight |
352.47
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| Exact Mass |
352.236
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| CAS # |
57469-77-9
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| Related CAS # |
Ibuprofen;15687-27-1
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| PubChem CID |
9841440
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| Appearance |
White to off-white solid powder
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| Boiling Point |
319.6ºC at 760 mmHg
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| LogP |
3.915
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
25
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| Complexity |
309
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| Defined Atom Stereocenter Count |
1
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| InChi Key |
IHHXIUAEPKVVII-ZSCHJXSPSA-N
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| InChi Code |
1S/C13H18O2.C6H14N2O2/c1-9(2)8-11-4-6-12(7-5-11)10(3)13(14)15;7-4-2-1-3-5(8)6(9)10/h4-7,9-10H,8H2,1-3H3,(H,14,15);5H,1-4,7-8H2,(H,9,10)/t;5-/m.0/s1
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| Chemical Name |
L-Lysine mono(4-isobutyl-alpha-methylbenzeneacetate)
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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 | 2.8371 mL | 14.1856 mL | 28.3712 mL | |
| 5 mM | 0.5674 mL | 2.8371 mL | 5.6742 mL | |
| 10 mM | 0.2837 mL | 1.4186 mL | 2.8371 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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