Naproxen etemesil [385800-16-8]
Cat# HY-19675-100mg
Size : 100mg
Brand : MedChemExpress
Naproxen etemesil is a lipophilic, non-acidic, inactive proagent of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
For research use only. We do not sell to patients.
Naproxen etemesil Chemical Structure
CAS No. : 385800-16-8
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This product is a controlled substance and not for sale in your territory.
Biological Activity
Protocol
Purity & Documentation
References
Customer Review
Naproxen etemesil is a lipophilic, non-acidic, inactive proagent of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay. | IC50: 8.72 μM (COX-1), 5.15 μM (COX-2) | |||||||||||||||
In Vitro | Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a well known nonsteroidal anti-inflammatory drug. Naproxen is approximately equipotent inhibitor of COX-1 and COX-2 in intact cells with IC50s of 2.2 μg/mL and 1.3 μg/mL, respectively. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. | |||||||||||||||
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In Vivo | Naproxen exerts an anti-inflammatory and antifibrotic effect in mouse model of bleomycin-induced lung fibrosis. Naproxen also downregulates TGF-β levels and Smad3/4 complex formation. Naproxen is shown to inhibit the time-courses of pain, fever and PGE2 with similar potencies (IC50=27, 40, 13 μM). MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. | |||||||||||||||
336.40 | ||||||||||||||||
C17H20O5S | ||||||||||||||||
385800-16-8 | ||||||||||||||||
Solid | ||||||||||||||||
White to off-white | ||||||||||||||||
O=C(OCCS(C)(=O)=O)[C@@H](C)C1=CC2=CC=C(OC)C=C2C=C1 | ||||||||||||||||
Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
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In Vitro: DMSO : 100 mg/mL (297.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing Stock Solutions
View the Complete Stock Solution Preparation Table * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo: Select the appropriate dissolution method based on your experimental animal and administration route. For the following dissolution methods, please ensure to first prepare a clear stock solution using an and then sequentially add co-solvents:
In Vivo Dissolution Calculator Please enter the basic information of animal experiments: Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments. Please enter your animal formula composition: % DMSO + % + % Tween-80 + % Saline The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE). Calculation results: Working solution concentration: mg/mL Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL). The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE). Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline. If the continuous dosing period exceeds half a month, please choose this protocol carefully. Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution. | ||||||||||||||||
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BAEC are incubated for 30 min with Naproxen (0.1 ng/mL to 1 mg/mL). Arachidonic acid (30 μM) is then added, and the cells are incubated for a further 15 min at 37°C. The medium is then removed, and radioimmunoassay is used to measure the formation of 6-keto-PGF,a, PGE2, thromboxane B2, or PGF2a. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
Rats To measure the analgesic effects of naproxen in a carrageenaninduced model of monoarthritis, Male Sprague–Dawley rats (n=48, 217±28 g) are randomly divided into four groups of 12 by an internally developed computer program, allowing the blind performance of the behavioral experiment. To induce hyperalgesia by inflammation, animals in groups 1B, 1C, and 1D receive a 40-μL intra-articular injection of a saline solution containing 7.5 mg/mL carrageenan in the left hind limb under isoflurane anesthesia (time=−1 h). Animals in group 1A receive no injection. After 1 h (time=0) the animals in groups 1A, 1B, 1C, and 1D receive oral doses of naproxen in saline of 0, 0, 7.5 and 30 μmol/kg, respectively. The doses and time points of measurements are selected on the basis of simulations predicting measuring a full concentration-effect relationship within the time-span of the experiment. Mice Bleomycin (0.05 IU) is instilled intratracheally to C57BL/6 mice, which are then treated by micro-osmotic pump with vehicle, JNJ7777120 (40 mg/kg b.wt.), naproxen (21 mg/kg b.wt.), or a combination of both. Airway resistance to inflation, an index of lung stiffness, is assessed, and lung specimens are processed for inflammation, oxidative stress, and fibrosis markers. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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[1]. Mitchell JA, et al. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proc Natl Acad Sci U S A. 1993 Dec 15;90(24):11693-7.
[2]. Rosa AC, et al. Prevention of bleomycin-induced lung inflammation and fibrosis in mice by naproxen and JNJ7777120 treatment. J Pharmacol Exp Ther. 2014 Nov;351(2):308-16.
[3]. Krekels EH, et al. Pharmacokinetic-pharmacodynamic modeling of the inhibitory effects of naproxen on the time-courses of inflammatory pain, fever, and the ex vivo synthesis of TXB2 and PGE2 in rats.
* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.9727 mL | 14.8633 mL | 29.7265 mL | 74.3163 mL |
5 mM | 0.5945 mL | 2.9727 mL | 5.9453 mL | 14.8633 mL | |
10 mM | 0.2973 mL | 1.4863 mL | 2.9727 mL | 7.4316 mL | |
15 mM | 0.1982 mL | 0.9909 mL | 1.9818 mL | 4.9544 mL | |
20 mM | 0.1486 mL | 0.7432 mL | 1.4863 mL | 3.7158 mL | |
25 mM | 0.1189 mL | 0.5945 mL | 1.1891 mL | 2.9727 mL | |
30 mM | 0.0991 mL | 0.4954 mL | 0.9909 mL | 2.4772 mL | |
40 mM | 0.0743 mL | 0.3716 mL | 0.7432 mL | 1.8579 mL | |
50 mM | 0.0595 mL | 0.2973 mL | 0.5945 mL | 1.4863 mL | |
60 mM | 0.0495 mL | 0.2477 mL | 0.4954 mL | 1.2386 mL | |
80 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9290 mL | |
100 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7432 mL |
- Immunology/Inflammation
- COX
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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Naproxen etemesil385800-16-8LT-NS 001 MX 1094MX1094MX 1094MX-1094COXCyclooxygenaseInhibitorinhibitorinhibit
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