EtoricoxibSpecific COX-2 inhibitor CAS# 202409-33-4 |
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Quality Control & MSDS
3D structure
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| Cas No. | 202409-33-4 | SDF | Download SDF |
| PubChem ID | 123619 | Appearance | Powder |
| Formula | C18H15ClN2O2S | M.Wt | 358.84 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | MK-663; MK-0663 | ||
| Solubility | DMSO : 100 mg/mL (278.68 mM; Need ultrasonic) | ||
| Chemical Name | 5-chloro-2-(6-methylpyridin-3-yl)-3-(4-methylsulfonylphenyl)pyridine | ||
| SMILES | CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl | ||
| Standard InChIKey | MNJVRJDLRVPLFE-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C18H15ClN2O2S/c1-12-3-4-14(10-20-12)18-17(9-15(19)11-21-18)13-5-7-16(8-6-13)24(2,22)23/h3-11H,1-2H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Etoricoxib(MK-0663) selectively inhibited COX-2 in human whole blood assays in vitro, with an IC50 value of 1.1 ± 0.1 μM for COX-2 (LPS-induced prostaglandin E2 synthesis), compared with an IC50 value of 116 ± 8 μM for COX-1 (serum thromboxane B2 generation after clotting of the blood).
IC50 value: 1.1 uM (LPS-induced prostaglandin E2 synthesis)
Target: COX-2
In summary, Etoricoxib represents a novel agent that selectively inhibits COX-2 with 106-fold selectivity in human whole blood assays in vitro and with the lowest potency of inhibition of COX-1 compared with other reported selective agents. Single preoperative oral dose (120 mg) of Etoricoxib, given one hour before surgery, has significantly reduced the post operative pain at rest and movement and improved sleep in patients undergoing single level diskectomy without any side effects and with good patient satisfaction. References: | |||||
Etoricoxib Dilution Calculator
Etoricoxib Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7868 mL | 13.9338 mL | 27.8676 mL | 55.7351 mL | 69.6689 mL |
| 5 mM | 0.5574 mL | 2.7868 mL | 5.5735 mL | 11.147 mL | 13.9338 mL |
| 10 mM | 0.2787 mL | 1.3934 mL | 2.7868 mL | 5.5735 mL | 6.9669 mL |
| 50 mM | 0.0557 mL | 0.2787 mL | 0.5574 mL | 1.1147 mL | 1.3934 mL |
| 100 mM | 0.0279 mL | 0.1393 mL | 0.2787 mL | 0.5574 mL | 0.6967 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Etoricoxib selectively inhibited COX-2 in human whole blood assays in vitro, with an IC50 value of 1.1 ± 0.1 μM for COX-2 (LPS-induced prostaglandin E2synthesis), compared with an IC50 value of 116 ± 8 μM for COX-1 (serum thromboxane B2 generation after clotting of the blood). In summary, Etoricoxib represents a novel agent that selectively inhibits COX-2 with 106-fold selectivity in human whole blood assays in vitro and with the lowest potency of inhibition of COX-1 compared with other reported selective agents. Single preoperative oral dose (120 mg) of Etoricoxib, given one hour before surgery, has significantly reduced the post operative pain at rest and movement and improved sleep in patients undergoing single level diskectomy without any side effects and with good patient satisfaction.
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Seizure following the Use of the COX-2 Inhibitor Etoricoxib.[Pubmed:28210513]
Case Rep Neurol Med. 2017;2017:1410759.
We describe a case of epileptic seizures occurring after the use of a COX-2 inhibitor. A 61-year-old man was admitted to our department because of a generalized tonic-clonic seizure. EEG showed generalized slowdown of the activity. Neuroimaging and blood samples studies did not evidence alterations, but a careful pharmacological history revealed that the patient had taken the COX-2 inhibitor Etoricoxib to treat lumbago few days before the onset of clinical symptoms. No seizures were reported after Etoricoxib discontinuation and an EEG resulted to be normal two months after this. Conclusion. Knowing the pharmacological history of a patient is important for understanding the clinical presentation and selecting appropriate treatment. This is, to the best of our knowledge, the first reported case of generalized seizures associated with the use of COX-2 inhibitors.
[The efficacy and safety of etoricoxib versus meloxicam in the treatment of patients with gonarthrosis].[Pubmed:28139564]
Ter Arkh. 2016;88(12):78-81.
AIM: To evaluate the clinical efficacy and tolerability of Etoricoxib and meloxicam in patients with gonarthrosis. SUBJECTS AND METHODS: A postregistration, open-labeled, prospective, comparative randomized study was conducted. 40 patients aged 37 to 75 years with primary knee osteoarthritis were examined. Therapeutic effectiveness was evaluated determining the functional index WOMAC with the use of a visual analogue scale (VAS). The tolerability of the drugs was assessed according to the opinions of a patient and a physician. RESULTS: Both drugs caused a reduction in WOMAC and VAS scores for pain and the severity of the disease. Etoricoxib demonstrated a significantly high rate of occurrence and completeness of its analgesic effect. Meloxicam showed a less pronounced decrease in joint stiffness and an insufficient analgesic effect. The incidence of side effects was similar in both groups. CONCLUSION: Both drugs demonstrated a good tolerability and a low incidence of side effects. The efficacy of Etoricoxib was significantly higher than that of meloxicam.
Design, synthesis and biological screening of some novel celecoxib and etoricoxib analogs with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile.[Pubmed:28057325]
Bioorg Chem. 2017 Feb;70:173-183.
Two new series of 4,6-diaryl-3-cyanopyridine 4a-r and 1,3,5-triaryl-2-pyrazolines 6a-f and were prepared. The new compounds were evaluated for their in vitro COX-2 selectivity and in vivo anti-inflammatory activity. Compounds 4o,r and 6d,f had moderate to high selectivity index (S.I.) compared to celecoxib (selectivity indexes of 4.5, 3.14, 4.79 and 3.21, respectively) and also, showed in vivo anti-inflammatory activity approximately equal to or higher than celecoxib (edema inhibition %=60.5, 64.5, 59.3 and 59.3, after 3h, respectively) and the effective anti-inflammatory doses were (ED50=10.1, 7.8, 8.46 and 10.7mg/kg respectively, celecoxib ED50=10.8mg/kg) and ulcerogenic liability were determined for these compounds which showed promising activity by being more potent than celecoxib with nearly negligible ulcerogenic liability compared to celecoxib (reduction in ulcerogenic liability versus celecoxib=85, 82, 74 and 67%, respectively).
