| Size | Price | |
|---|---|---|
| 10mg | ||
| 25mg | ||
| 50mg | ||
| 100mg |
Ketoprofen lysine salt is the lysine salt form of ketoprofen which is a nonsteroidal anti-inflammatory drugs (NSAID) with analgesic and antipyretic effects. It acts by inhibiting the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). Potential use in inflammation, immunology, and metabolic disease such as obesity.
| Targets |
|
|
|---|---|---|
| ln Vitro |
In LPS-stimulated monocytes isolated from human blood, ketoprofen lysinate inhibits COX with IC50 values of 2 nM (COX-1) and 26 nM (COX-2)[1]. TNFα, IL-8, SAA, COX-2, and PTGES mRNA levels are reduced in LPS-stimulated bovine mammary epithelial cells when treated with 2.5 mg/mL ketoprofen lysinate for 3–24 hours[3].
|
|
| ln Vivo |
In HFD-induced obese C57BL/6 mice, ketoprofen lysinate (oral treatment, 10 mg/kg, three times a week for 10 weeks) reduces relative body weight (15.41%), iWAT mass (about 41%), and the levels of leptin (58.68%) and resistin (12.88%)[2]. In dairy cows exposed with lipopolysaccharide (LPS), 50 mg/kg of ketoprofen lysinate reduces the rise in somatic cell count (SCC), serum albumin (SA), immunoglobulin G, and lactate dehydrogenase (LDH) activity in milk[3].
|
|
| Cell Assay |
RT-PCR[3]
Cell Types: LPS (0.2 μg/mL)- stimulated bovine mammary epithelial cells Tested Concentrations: 2.5 mg /mL Incubation Duration: 3, 6, 24 h Experimental Results: diminished the mRNA level of TNFα, IL-8, SAA, COX-2 and PTGES. |
|
| Animal Protocol |
Animal/Disease Models: HFD-induced obese C57BL/6 mice[2]
Doses: 10 mg/kg Route of Administration: Oral administration, three times a week for 10 weeks Experimental Results: diminished in relative body weight , the iWAT mass, and the level of leptin and resistin. Animal/Disease Models: LPS (0.2 μg/mL)-treated dairy cows [3] Doses: 50 mg/kg Route of Administration: Injection (Milk samples were taken every 30 min until 6 and 9 h) Experimental Results: Lowered the increase of somatic cell count (SCC), serum albumin (SA), IgG and lactate dehydrogenase (LDH) activity in milk. |
|
| References |
[1]. Palomer A, et al. Structure-based design of cyclooxygenase-2 selectivity into ketoprofen. Bioorg Med Chem Lett. 2002 Feb 25;12(4):533-7.
[2]. NamHyeon Kang Ketoprofen alleviates diet-induced obesity and promotes white fat browning in mice via the activation of COX-2 through mTORC1-p38 signaling pathway. Pflugers Arch. 2020 May;472(5):583-596. [3]. Denisa Dan, et al. Ketoprofen affects the mammary immune response in dairy cows in vivo and in vitro. J Dairy Sci. 2018 Dec;101(12):11321-11329. |
| Molecular Formula |
C16H14O3.C6H14N2O2
|
|---|---|
| Molecular Weight |
400.47
|
| CAS # |
57469-78-0
|
| Related CAS # |
Ketoprofen;22071-15-4
|
| SMILES |
NCCCC[C@@H](C(=O)O)N.OC(C(C1C=CC=C(C(C2=CC=CC=C2)=O)C=1)C)=O
|
| 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 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 | 2.4971 mL | 12.4853 mL | 24.9707 mL | |
| 5 mM | 0.4994 mL | 2.4971 mL | 4.9941 mL | |
| 10 mM | 0.2497 mL | 1.2485 mL | 2.4971 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
