| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Other Sizes |
| Targets |
NS-398 is a selective inhibitor of COX-2 with an IC50 of 3.8 μM. It has no effect on COX-1 at concentrations up to 100 μM. This specificity makes it a useful tool for studying the role of COX-2 in prostaglandin synthesis and inflammation.
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| ln Vitro |
Non-steroidal anti-inflammatory drug NS-398 acts as an antagonist of G/H synthase/cyclooxygenase (COX-2) and has no effect on COX-1 at 100 μM. Its IC50 is 3.8 μM. [1]. Sheep seminal vesicle microsomes exhibit a weak inhibition of PG endoperoxide synthase activity by NS-398 (IC50: 11 μM)[2].
In vitro, NS-398 selectively inhibits COX-2 activity (IC50 = 3.8 μM) with no effect on COX-1 at 100 μM. It is a non-steroidal anti-inflammatory agent with analgesic and antipyretic effects. The compound is used to study the differential roles of COX-1 and COX-2 in inflammation and pain. |
| ln Vivo |
NS-398 (0.5–10 mg/kg, po) had an antipyretic and rotational sedative effect (ED50, 1.84 mg/kg), as well as an efficacious venous return amyloid (ED30, 1.14 mg/kg) and effective management of auxiliary arthritis (ED 30, 4.69 mg/kg). With an ED50 of 8.2 mg/kg, NS-398 GFP induced a writhing reaction in mice [2].
In vivo, NS-398 is an orally bioavailable nonsteroidal anti-inflammatory compound. It functions as a selective inhibitor of COX-2 in inflammatory tissues and exhibits minimal inhibitory activity against COX-1 in gastric tissues. The compound has been studied for its analgesic and antipyretic properties. |
| Enzyme Assay |
In vitro enzyme assays for NS-398 typically measure its ability to inhibit COX-1 and COX-2 activity. The enzymes are incubated with arachidonic acid in the presence of increasing concentrations of the compound. The formation of prostaglandins is measured by ELISA or radioimmunoassay. IC50 values are calculated from dose-response curves. Selectivity is assessed by comparing IC50 values for COX-1 and COX-2.
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| Cell Assay |
Cell-based assays for NS-398 involve treating inflammatory cells (e.g., macrophages, monocytes) with the compound and measuring prostaglandin E2 (PGE2) production. Cells are stimulated with LPS or other inflammatory stimuli in the presence and absence of the compound. PGE2 levels in the culture supernatant are measured by ELISA. The compound's ability to inhibit COX-2-mediated PGE2 production is quantified.
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| Animal Protocol |
In vivo animal studies for NS-398 typically involve administering the compound to rodent models of inflammation (e.g., carrageenan-induced paw edema, air pouch model). The compound is given orally or intraperitoneally. Inflammatory markers (e.g., PGE2 levels, edema) are measured. The compound's anti-inflammatory and analgesic effects are assessed. Gastric mucosal integrity is evaluated to confirm COX-1 sparing.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NS-398 are characteristic of orally bioavailable NSAIDs. The compound is absorbed following oral administration and distributed to tissues. It accumulates in inflammatory tissues where COX-2 is upregulated. Metabolism occurs primarily in the liver. Excretion occurs through renal pathways. The compound's half-life is suitable for anti-inflammatory applications.
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| Toxicity/Toxicokinetics |
Toxicological profile of NS-398 is favorable compared to non-selective NSAIDs due to its COX-2 selectivity. The compound causes minimal gastric irritation and ulceration. Common side effects include mild gastrointestinal disturbances. The compound's COX-2 selectivity reduces the risk of gastric toxicity but may increase the risk of cardiovascular events with long-term use. The safety profile is consistent with selective COX-2 inhibitors.
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| References |
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| Additional Infomation |
NS-398 is a C-nitro compound with the structure N-methylsulfonyl-4-nitroaniline, containing an additional cyclohexyloxy substituent at the 2-position. It is a cyclooxygenase 2 inhibitor and an antitumor drug. It is a sulfonamide, aromatic ether, and C-nitro compound. Its function is similar to 4-nitroaniline. NS-398 is a COX-2 inhibitor. It was developed as part of research into the mechanism of cyclooxygenase. It has been reported that Plantago major contains N-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide, and related data have been reported.
NS-398 is a widely used research tool for studying the role of COX-2 in inflammation, pain, and cancer. It is a selective COX-2 inhibitor that is used to differentiate the effects of COX-1 and COX-2 inhibition. The compound is not approved for clinical use but is a valuable reagent for preclinical research. |
| Molecular Formula |
C13H18N2O5S
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|---|---|
| Molecular Weight |
314.36
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| Exact Mass |
314.093
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| CAS # |
123653-11-2
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| PubChem CID |
4553
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
490.6±55.0 °C at 760 mmHg
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| Melting Point |
139 °C
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| Flash Point |
250.5±31.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.593
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| LogP |
3.67
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
450
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| Defined Atom Stereocenter Count |
0
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| SMILES |
0
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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 |
| 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 : ~33.33 mg/mL (~106.02 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.95 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. Solubility in Formulation 2: ≥ 1.67 mg/mL (5.31 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 16.7 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. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1811 mL | 15.9053 mL | 31.8107 mL | |
| 5 mM | 0.6362 mL | 3.1811 mL | 6.3621 mL | |
| 10 mM | 0.3181 mL | 1.5905 mL | 3.1811 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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