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| 5g |
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| 25g |
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Purity: ≥98%
Naproxen (also known as (S)-Naproxen)) is a non-steroidal anti-inflammatory drug (NSAID) which is a nonselective COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively. Naproxen is approximately equipotent inhibitor of COX-1 and COX-2 in intact cells with IC50 of 2.2 μg/mL and 1.3 μg/mL, respectively. Naproxen decreases the in vitro LPS-induced PGE2 and TXB2 production in rats and humans with IC50 of 30.7 μM and 79.5 μM for PGE2 inhibition, 72.4 μM and 48.3 μM for TXB2 inhibition, respectively.
| ln Vitro |
Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that, when absorbed, hydrolyzes to produce naproxen that is pharmacologically active. One well-known non-steroidal anti-inflammatory medication is naproxen. With IC50s of 2.2 μg/mL and 1.3 μg/mL, respectively, naproxen is a nearly equal inhibitor of COX-1 and COX-2 in intact cells [1].
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| ln Vivo |
Naproxen reduces inflammation and inhibits fibrosis in a mouse model of lung fibrosis caused by bleomycin. Additionally, naproxen inhibits the production of the Smad3/4 complex and TGF-β levels [2]. Similar potency (IC50=27, 40, 13 μM) was shown in the time course suppression of pain, fever, and PGE2 by naproxen [3].
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| References |
[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 |
| Molecular Formula |
C14H14O3
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|---|---|
| Molecular Weight |
230.2592
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| Exact Mass |
230.0943
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| CAS # |
22204-53-1
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| Related CAS # |
(±)-Naproxen;23981-80-8;Naproxen sodium;26159-34-2
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| SMILES |
O=C(O)[C@@H](C)C1=CC=C2C=C(OC)C=CC2=C1
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| InChi Key |
CMWTZPSULFXXJA-VIFPVBQESA-N
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| InChi Code |
InChI=1S/C14H14O3/c1-9(14(15)16)10-3-4-12-8-13(17-2)6-5-11(12)7-10/h3-9H,1-2H3,(H,15,16)/t9-/m0/s1
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| Chemical Name |
(S)-2-(6-methoxynaphthalen-2-yl)propanoic acid
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| Synonyms |
CG 3117 CG3117 CG-3117 Naproxen Naposin Napratec
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~434.29 mM)
H2O : ~75 mg/mL (~325.72 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.86 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 (10.86 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 (10.86 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: 2 mg/mL (8.69 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 | 4.3429 mL | 21.7146 mL | 43.4292 mL | |
| 5 mM | 0.8686 mL | 4.3429 mL | 8.6858 mL | |
| 10 mM | 0.4343 mL | 2.1715 mL | 4.3429 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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