| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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| 25g |
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Purity: ≥98%
Nimesulide (formerly R-805; R 805; R805), a non-steroidal anti-inflammatory drug (NSAID), is a potent and selective COX-2 inhibitor with analgesic and antipyretic properties. It inhibits COX-2 with an IC50 of 26 μM. Nimesulide has been approved for the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old. It works by blocking the production of prostaglandins (a chemical associated with pain) thereby relieving pain and inflammation.
| ln Vitro |
Nimesulide exhibits a limited effect on COX-1 (IC50 >100 μM), but it is a selective inhibitor of COX-2 with IC50s ranging from 70 nM to 70 μM in a time-dependent manner[1]. In endometrial cancer cells, imimezolide (10 μM) significantly reduces VEGF, while having no effect on normal cells. Nimesulide (10 and 50 µM) significantly lowers MCP-1 levels in normal cells; 10 µM has the same effect on cancer cells. Moreover, mesulide (50 µM) has little effect on cancer cells but has a strong effect on the amount of IL-8 in normal cells[3].
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| ln Vivo |
In rats, imesulide (3 and 10 mg/kg, ip) significantly prevents fever brought on by an intraperitoneal injection of LPS. Nimesulide (3 mg/kg, ip) potently suppresses the fever response brought on by TNF-α, IL-1β, or IL-6, but it has no effect on the arachidonic acid-induced initial spike in the fever response. Additionally, mesulide dramatically lowers PGE2 and PGF2α levels in the brain fluid of rats treated with lipopolysaccharide (LPS) and 97% suppresses the rise in plasma TNF-α[2].
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| Animal Protocol |
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| References |
[1]. Vago T, et al. Effect of nimesulide action time dependence on selectivity towards prostaglandin G/H synthase/cyclooxygenase activity. Arzneimittelforschung. 1995 Oct;45(10):1096-8.
[2]. Werner MF, et al. Nimesulide-induced antipyresis in rats involves both cyclooxygenase-dependent and independent mechanisms. Eur J Pharmacol. 2006 Aug 14;543(1-3):181-9. [3]. Genç S, et al. The effect of COX-2 inhibitor, nimesulide, on angiogenetic factors in primary endometrial carcinoma cell culture. Clin Exp Med. 2007 Mar;7(1):6-1 |
| Molecular Formula |
C13H12N2O5S
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| Molecular Weight |
308.31
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| CAS # |
51803-78-2
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| Related CAS # |
Nimesulide-d5;1330180-22-7
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| SMILES |
S(C([H])([H])[H])(N([H])C1C([H])=C([H])C(=C([H])C=1OC1C([H])=C([H])C([H])=C([H])C=1[H])[N+](=O)[O-])(=O)=O
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| InChi Key |
HYWYRSMBCFDLJT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H12N2O5S/c1-21(18,19)14-12-8-7-10(15(16)17)9-13(12)20-11-5-3-2-4-6-11/h2-9,14H,1H3
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| Chemical Name |
N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2435 mL | 16.2174 mL | 32.4349 mL | |
| 5 mM | 0.6487 mL | 3.2435 mL | 6.4870 mL | |
| 10 mM | 0.3243 mL | 1.6217 mL | 3.2435 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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