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Synonyms | RS-3650 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C14H13NaO3 |
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分子量 | 252.24 | CAS No. | 26159-34-2 | |
Solubility (25°C)* | 体外 | Water | 50 mg/mL (198.22 mM) | |
DMSO | 10 mg/mL (39.64 mM) | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Naproxen Sodium (RS-3650) is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively. |
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in vitro | 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. [1] 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. [2] Naproxen produces concentration-related inhibition of TXB2 production from human platelets and LPS-induced TXB2 production from human mononuclear cells with plC50 values (-log concentration inhibiting TXB2 by 50%) of 5.7 and 6.4, respectively, and exhibits slightly inhibitory selectivity for constitutive and induced COX-2 with IC50 COX-1/IC50 COX-2 of 6.3. [3] Only high concentration of Naproxen can significantly induce apoptosis at 48 hours in HCA-7 colon cancer cells with IC50 of 1.45 mM. [4] |
in vivo | Administration of Naproxen reduces the LPS-induced PGE2 and TXB2 production in vivo in rats with IC50 values of 12.8 μM and 5.9 μM, respectively, which represents that Naproxen is a nonselective COX inhibitor with the log IC50 ratio (COX-2/COX-1) of 0.34. [2] Naproxen displays IC50 of 27 μM for analgesia in a rat model with carrageenan-induced arthritis and IC50 of 40 μM for antipyretics in a yeast-induced fever rat model, while exhibits inhibition of PGE2 with IC50 of 13 μM and TXB2 with IC50 of 5 μM. [5] |
特徴 | Displays approximately equipotent inhibitory selectivity for COX-1 and COX-2 in intact cells. |
キナーゼアッセイ | COX-1 and COX-2 activities in intact cells | |
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For the determination of COX-1 and COX-2 inhibition, bovine aortic endothelial cells (BAEC) are incubated for 30 minutes with Naproxen (0.1 ng/mL to 1 mg/mL), and cultured J774.2 macrophages are treated with endotoxin at 1 μg/mL for 12 hours to induce COX-2 followed by incubated for 30 minutes with Naproxen (0.1 ng/mL to 1 mg/mL), respectively. Arachidonic acid (30 μM) is then added, and the cells are incubated for a further 15 minutes at 37 °C. The medium is then removed, and radioimmunoassay is used to measure the formation of 6-keto-PGF1α, PGE2, thromboxane B2, or PGF2α for the assessment of IC50 for COX-1 and COX-2. | ||
細胞アッセイ | 細胞株 | Human colon cancer HCA-7 cell lines |
濃度 | Dissolved in culture medium, final concentration ~20 mM | |
反応時間 | 24 and 48 hours | |
実験の流れ | Cells are exposed to Naproxen for 24 and 48 hours, respectively. At the end of incubation, cells are harvested by trypsinization, stained with trypan blue solution (0.04% wt/vol) and counted in a Neubauer haemocytometer chamber for the determination of cell viability. | |
動物実験 | 動物モデル | Male Sprague-Dawley rats |
投薬量 | 2.5, 10 or 25 mg/kg | |
投与方法 | Intravenously (i.v.) infusion or intraperitoneal (i.p.) injection |
Project IDentif.AI: Harnessing Artificial Intelligence to Rapidly Optimize Combination Therapy Development for Infectious Disease Intervention [ Adv Ther (Weinh), 2020, 2000034] | PubMed: 32838027 |
Strain-Dependent Variability of Early Discovery Small Molecule Pharmacokinetics in Mice: Does Strain Matter? [ Drug Metab Dispos, 2020, 48(8):613-621] | PubMed: 32474442 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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