Imrecoxib
Imrecoxib
CAS: 395683-14-4
Molecular Formula: C21H23NO3S
Imrecoxib - Names and Identifiers
| Name | Imrecoxib |
| Synonyms | Imrecoxib 2H-Pyrrol-2-one, 1,5-dihydro-3-(4-methylphenyl)-4-[4-(methylsulfonyl)phenyl]-1-propyl- |
| CAS | 395683-14-4 |
Imrecoxib - Physico-chemical Properties
| Molecular Formula | C21H23NO3S |
| Molar Mass | 369.48 |
| Density | 1?+-.0.06 g/cm3(Predicted) |
| Boling Point | 604.1±55.0 °C(Predicted) |
| pKa | -2.25±0.60(Predicted) |
| Storage Condition | 2-8°C，干燥，密封 |
Imrecoxib - Reference Information
| Non-steroidal anti-inflammatory drugs | imrecoxib is a non-steroidal anti-inflammatory drugs (NSAIDs), according to the concept of "moderate inhibition" of COX-2, the selective COX-2 inhibitors were independently developed by Institute of Materia Medica, Chinese Academy of Medical Sciences and Jiangsu Hengrui Pharmaceutical Co., Ltd, it is desirable to reduce the chance of gastrointestinal irritation and cardiovascular damage while suppressing inflammation and pain. The drug was approved by the State Food and Drug Administration (SFDA) on May 20, 2011. However, since the national innovative drug policy was not perfect at that time, the post-marketing sales of imrecoxib was not optimistic. It was not until that the market entered the national health insurance, and the market was rapidly expanding, with sales of 0.369 billion yuan in 2018, the increase was as high as 64.79%. This product is used to relieve pain symptoms of osteoarthritis. Only applicable to men and women of non-childbearing age who do not require childbearing. |
| indications | imrecoxib is indicated for the relief of painful symptoms of osteoarthritis in men and in women of non-childbearing age who do not require fertility. Avoid co-administration with other NSAIDs, including selective COX-2 inhibitors. This product can not be used to replace corticosteroids or treatment of corticosteroid hormone deficiency. |
| preparation | starting with 2-[4-(methylsulfonyl) phenyl] oxirane (2), N-N-propyl-β-hydroxy-4-methanesulfonylphenethylamine (3) is formed by addition ring opening; N-N-propyl-N-[2-hydroxy-2-(4-methanesulfonylphenyl)] (N-propyl-N-[2-hydroxy-2-(4-methanesulfonylphenyl)) is produced by condensation of 3 with 4-methylphenylacetic acid via acid amine in the presence of condensation agent carbonyl diimidazole.] ethyl -4-Methyl phenyl acetamide (4), simple operation, the yield of 98%;4 by Jone's reagent oxidation, in potassium carbonate/ethanol/water system Ring 1, the reaction time was shortened from 8H to 2H, and the yield was increased from 61% to 78%. At the same time, the post-treatment was simplified and the appearance of the product was improved. The overall yield was 38.5% (based on 2), which was 12% higher than that in the literature. |
| drug interaction | the interaction of imrecoxib with other drugs has not been studied systematically. The results of in vitro enzyme inhibition experiments showed that it had weak inhibitory effect on CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4. |
| side effects and adverse reactions | Imrecoxib Tablets of side effects rarely occur, may cause serious cardiovascular adverse reactions, for example, myocardial infarction or stroke. May cause gastrointestinal discomfort, rare and more serious adverse reactions such as ulcers and bleeding, patients should be alert to the symptoms and signs of ulcers and bleeding, seek medical help when discovering any signs and symptoms that predict these disorders, including epigastric pain, indigestion, Melena, and hematemesis. coxib belongs to a class of hot drugs for the treatment of arthritis in clinic. Compared with traditional non-steroidal anti-inflammatory drugs, it has less adverse reactions to the digestive system. Coxib drugs have attracted much attention since their birth. Rofecoxib, Valdecoxib and romexoxib were successively withdrawn from the market in 2004 due to adverse cardiovascular reactions, the safety of coxib drugs has been debated. At present, the main clinical varieties are celecoxib, parecoxib, ecoxib, valdecoxib, lumicoxib and so on. |
| biological activity | Imrecoxib(BAP-909) Imrecoxib is a selective cyclooxygenase 2 (COX-2) inhibitor, the IC50 value is 18 nM, which can also inhibit COX1 activity, and the IC50 value is 115 nM. Imrecoxib(BAP-909) Imrecoxib has an anti-inflammatory effect. |
| Cell Line: | U937 cells |
| Concentration: | 0.1 µM; 1 µM; 10 µM |
| Incubation Time: | 24 hours |
| Result: | Decreased COX-2 mRNA level. Inhibited the edema response with different doses. Inhibited adjuvant-induced chronic inflammation at the doses of 10 and 20 mg/kg. |
| Animal Model: | Rat carrageenan-induced edema model [1] Rat adjuvant-induced arthritis (AIA) model [1] |
| Dosage: | 5 mg/kg, 10 mg/kg, 20 mg/kg 5 mg/kg, 10 mg/kg, 20 mg/kg |
| Administration: | Gastrointestinal administration; 5-20 mg/kg; 1 hour before carrageenan injection Gastrointestinal administration; 5-20 mg/kg; started on day 7; 26 days |
Last Update：2024-04-09 02:00:14
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