Drug
D0092 | Nimesulide
M
M02AA26 Nimesulide
[M02AA] Antiinflammatory preparations, non-steroids for topical use
[M02A] TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN
[M02] TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN
[M] Musculoskeletal system
M01AX17 Nimesulide
[M01AX] Other antiinflammatory and antirheumatic agents, non-steroids
[M01A] ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS
[M01] ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS
[M] Musculoskeletal system
| Toxicity | Dose | Time | Species | Model | Method | Action | Positive criterion | Reference |
|---|---|---|---|---|---|---|---|---|
| TRANSMEMBRANE POTENTIAL | 30 | 24hr | rat | hepatocytes | tetramethylrhodamine ethyl ester (TMRE) | decrease | AC50 (μM) | 40 |
| OPENING OF PERMEABILITY TRANSITION PORE (PTP) | 197 | |||||||
| UNCOUPLING | increase | 35 | ||||||
| UNCOUPLING | increase | 36 | ||||||
| UNCOUPLING | affect | 197 | ||||||
| UNCOUPLING | 197 | |||||||
| MEMBRANE POTENTIAL | 3.87±0.23 | human | qHTS-HepG2 | MMP assay | decrease | IC50 | 163 | |
| MEMBRANE POTENTIAL | 4.16 | human | HepG2 | MMP assay | decrease | IC50 | 163 | |
| MEMBRANE POTENTIAL | 2.74±0.35 | rat | hepatocytes | MMP assay | decrease | IC50 | 163 | |
| MEMBRANE POTENTIAL | 10.1 µM | 30 mins | mouse | liver mitochondria | Rh123 fluorescence (excitation 485 nm, emission 535 nm) are recorded using a fluorescence multi-well plate reader (mCICCP (20 µM) treatments was considered as the 100% baseline for ΔΨm loss) | decrease | EC20 | 36 |
| RESPIRATION | < 25 µM | 60 mins | mouse | liver mitochondria | Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. | decrease | EC20 | 36 |
| RESPIRATION | ND | 60 mins | mouse | liver mitochondria | Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. | Negative | EC20 | 36 |
| RESPIRATORY STATES | 197 | |||||||
| STATE 2 RESPIRATION | 2.6 ± 0.2 | rat | isolated rat liver mitochondria | State 2 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) | inhibit | UC50 (nmol/mg mitochondrial protein) | 40 | |
| STATE 3 RESPIRATION | 100 nmol/mg mitochondrial protein | rat | isolated rat liver mitochondria | State 3 respiration ( 96-well plate format using a phosphorescent oxygen-sensitive probe MitoXpress) | Negative | IC50 (nmol/mg mitochondrial protein) | 40 | |
| OXYGEN CONSUMPTION RATE (OCR) | 1 mM | rat; Sprague-Dawley Crl:CD (SD) BR | lung microsomes | measurement of oxygen consumption | increase | p < 0.05 | 11 | |
| LIPID METABOLISM | 29 | 24hr | rat | hepatocytes | LipidTox, for neutral lipid accumulation, to evaluate lipid content. | accumulation | AC50 (μM) | 40 |
| NADPH METABOLISM | 1 mM | rat; Sprague-Dawley Crl:CD (SD) BR | lung microsomes | measurement of NADPH oxidation | increase | p < 0.05 | 11 | |
| GLUTATHIONE METABOLISM | 1 | 24hr | rat | hepatocytes | glutathion depletion: cells were incubated with 50 μM monochlorobimane with 6 μg/ml Hoechst 33342 | AC50 (μM) | 40 | |
| SWELLING | 10 μM | 20 minutes | rat; Wistar; normal | liver mitochondria | Measurements of mitochondrial swelling | increase | ID50 | 12 |
| SWELLING | 7.3 μM | 20 minutes | rat; Wistar; arthritis | liver mitochondria | Measurements of mitochondrial swelling | increase | ID50 | 12 |
| SWELLING | > 200 µM | 30 mins | mouse | liver mitochondria | swelling assay: Absorbance at 545 nm using a fluorescence multi-well plate reader (CaCl2 (50 µM) was considered as the 100% baseline for the swelling ) | increase | EC20 | 36 |
| OXIDATIVE STRESS | 1 mM | rat; Sprague-Dawley Crl:CD (SD) BR | lung microsomes | adrenochrome assay (Misra and Fridovich, 1972) | increase | p < 0.05 | 11 | |
| OXIDATIVE STRESS | 0.5 mM | 20 minutes | rat; Sprague-Dawley Crl:CD (SD) BR | lung microsomes | horseadish preoxidase method (Green and Hill, 1984) | increase | p < 0.05 | 11 |
| ROS PRODUCTION | 574 | rat | hepatocytes | use CM-H2DCFDA to monitor reactive oxygen species | AC50 (μM) | 40 | ||
| CYTOCHROME C RELEASE | 21 | 24hr | rat | hepatocytes | cytochrome c release (anti-cytochrome c antibody ) | induce | AC50 (μM) | 40 |
| ER STRESS-INDUCED | 8 | 24hr | rat | hepatocytes | DNA damage 153 induction (GADD153 antibodies) for ER-stress induced apoptosis | induce | AC50 (μM) | 40 |
| Target | Dose | Time | Species | Model | Method | Action | Positive criterion | Reference |
|---|---|---|---|---|---|---|---|---|
| NADH:ubiquinone reductase | < 25 µM | 60 mins | mouse | liver mitochondria | Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. | inhibit | EC20 | 36 |
| Succinate dehydrogenase | ND | 60 mins | mouse | liver mitochondria | Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. | Negative | EC20 | 36 |
| superoxide | 1 mM | rat; Sprague-Dawley Crl:CD (SD) BR | lung microsomes | adrenochrome assay (Misra and Fridovich, 1972) | increase | p < 0.05 | 11 | |
| hydrogen peroxide | 0.5 mM | 20 minutes | rat; Sprague-Dawley Crl:CD (SD) BR | lung microsomes | horseadish preoxidase method (Green and Hill, 1984) | increase | p < 0.05 | 11 |
| Cytochrome c | > 200 µM | 30 mins | mouse | liver mitochondria | Cytochrome c release was evaluated using ELISA kit ( 20 µg/ml Alamethicin was used as 100% baseline) | release | EC20 | 36 |
| Pictogram | Signal | Statements | Precautionary Statement Codes |
|---|---|---|---|
  |
Danger |
Aggregated GHS information provided by 56 companies from 13 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies. Reported as not meeting GHS hazard criteria by 2 of 56 companies. For more detailed information, please visit ECHA C&L website Of the 12 notification(s) provided by 54 of 56 companies with hazard statement code(s): H301 (87.04%): Toxic if swallowed [Danger Acute toxicity, oral] H302 (12.96%): Harmful if swallowed [Warning Acute toxicity, oral] Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown. |
P264, P270, P301+P310, P301+P312, P321, P330, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.) |
| (methylsulfonyl)(4-nitro-2-phenoxyphenyl)amine | 4'-Nitro-2'-phenoxymethanesulfonanilide | 4'-Nitro-2'-phenoxymethansulfonanilid |
| 4-NITRO-2-PHENOXYMETHANESULFONANILIDE | 4-Nitro-2-phenoxy-methanesulfonanilide | 51803-78-2 |
| 803N782 | A828786 | AB00052332 |
| AB00052332-16 | AB00052332_17 | AB00052332_18 |
| AB2000444 | AC-4524 | AK163559 |
| AKOS015897356 | Aldoron | Antifloxil |
| Aulin | BCBcMAP01_000034 | BCP10076 |
| BDBM50056999 | BPBio1_000163 | BRD-K76775527-001-06-2 |
| BRD-K76775527-001-18-7 | BRN 2421175 | BSPBio_000147 |
| BSPBio_001103 | BSPBio_003112 | Bio2_000382 |
| Bio2_000862 | C13H12N2O5S | CAS-51803-78-2 |
| CCG-39319 | CCRIS 8225 | CHEBI:44445 |
| CHEMBL56367 | CN0038 | CS-2420 |
| Certified Reference Material | D01049 | DB-052029 |
| DB04743 | DSSTox_CID_17250 | DSSTox_GSID_37250 |
| DSSTox_RID_79316 | DTXSID3037250 | DivK1c_000693 |
| EI-287 | EINECS 257-431-4 | EU-0100855 |
| FT-0630650 | Flogovital | GTPL7401 |
| Guaxan | HMS1362G05 | HMS1568H09 |
| HMS1792G05 | HMS1922K17 | HMS1990G05 |
| HMS2089B14 | HMS2095H09 | HMS2234K19 |
| HMS3262L11 | HMS3269G17 | HMS3371J19 |
| HMS3403G05 | HMS3414P09 | HMS3649A04 |
| HMS3655D13 | HMS3678P07 | HMS3712H09 |
| HMS502C15 | HY-B0363 | HYWYRSMBCFDLJT-UHFFFAOYSA-N |
| IDI1_000693 | IDI1_002137 | KBio1_000693 |
| KBio2_000443 | KBio2_002057 | KBio2_003011 |
| KBio2_004625 | KBio2_005579 | KBio2_007193 |
| KBio3_000825 | KBio3_000826 | KBio3_002612 |
| KBioGR_000443 | KBioGR_000695 | KBioSS_000443 |
| KBioSS_002057 | KS-1277 | LP00855 |
| LS-90290 | Lopac-N-1016 | Lopac0_000855 |
| MCULE-4217888990 | MFCD00079470 | MLS000069680 |
| MLS001148268 | Mesulid | Methanesulfonamide, N-(4-nitro-2-phenoxyphenyl)- |
| Methanesulfonamide, N-(4-nitro-2-phenoxyphenyl)- (9CI) | Methanesulfonanilide, 4'-nitro-2'-phenoxy- | N 1016 |
| N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide | N-(4-nitro-2-phenoxy-phenyl)methanesulfonamide | N-(4-nitro-2-phenoxyphenyl) |
| N-[4-nitro-2-(phenoxy)phenyl]methanesulfonamide | N0984 | NCGC00015725-01 |
| NCGC00015725-02 | NCGC00015725-03 | NCGC00015725-04 |
| NCGC00015725-05 | NCGC00015725-06 | NCGC00015725-07 |
| NCGC00015725-08 | NCGC00015725-09 | NCGC00015725-10 |
| NCGC00015725-11 | NCGC00015725-12 | NCGC00015725-13 |
| NCGC00015725-15 | NCGC00015725-16 | NCGC00021842-03 |
| NCGC00021842-04 | NCGC00021842-05 | NCGC00021842-06 |
| NCGC00021842-07 | NCGC00021842-08 | NCGC00255661-01 |
| NCGC00261540-01 | NIM | NIM-03 |
| NINDS_000693 | NSC-758412 | NSC758412 |
| Nimed | Nimedex | Nimesulida |
| Nimesulida [INN-Spanish] | Nimesulide (JAN/INN) | Nimesulide [BAN:INN] |
| Nimesulide [INN:BAN] | Nimesulide for peak identification, European Pharmacopoeia (EP) Reference Standard | Nimesulide, European Pharmacopoeia (EP) Reference Standard |
| Nimesulide, Pharmaceutical Secondary Standard | Nimesulide,(S) | Nimesulidum |
| Nimesulidum [INN-Latin] | Nise Gel | Nisulid |
| Opera_ID_1247 | Orthobid | Pharmakon1600-01503231 |
| Prestwick0_000194 | Prestwick1_000194 | Prestwick2_000194 |
| Prestwick3_000194 | Prestwick_618 | Q20994 |
| R 805 | R-805 | SBI-0050831.P003 |
| SC-17925 | SCHEMBL24882 | SMR000058484 |
| SPBio_001382 | SPBio_002068 | SPECTRUM1503231 |
| SR-01000000218 | SR-01000000218-11 | SR-01000000218-2 |
| SR-01000000218-6 | SR-01000000218-7 | ST51015069 |
| STL018679 | SW196785-3 | Spectrum2_001541 |
| Spectrum3_001576 | Spectrum4_000178 | Spectrum5_000964 |
| Spectrum_001577 | Sulidene | Tox21_110207 |
| Tox21_110207_1 | Tox21_301850 | Tox21_500855 |
| UNII-V4TKW1454M | V4TKW1454M | W-105866 |
| ZINC4617749 | n-(4-nitro-2-phenoxy-phenyl)-methanesulfonamide | nimesulide |
| s2040 |
| DrugBank Name | Nimesulide |
| DrugBank | DB04743 |
| CAS Number | 1364966-82-4, 51803-78-2 |
| PubChem Compound | 4495 |
| KEGG Drug | D01049 |
| PubChem.Substance | 46507721 |
| ChEBI | 44445 |
| PharmGKB | PA137179528 |
| ChemSpider | 4339 |
| BindingDB | 50056999.0 |
| TTD | DPR000079 |
| Wikipedia | Nimesulide |
| HET | NIM |
1. Moreno-Sanchez et al. (1999)
2. Vuda et al. (2016)