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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Etoricoxib (also known as MK-0663) is a non-steroidal anti-inflammatory drgu (NSAID) which acts as a selective and orally bioactive COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood. Etoricoxib is a synthetic NSAID with antipyretic, analgesic, and potential antineoplastic properties. Etoricoxib binds specifically to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in inhibition of the conversion of arachidonic acid into prostaglandins. Inhibition of COX-2 may induce apoptosis and inhibit tumor cell proliferation and angiogenesis.
ln Vitro |
Etoricoxib, also known as MK-0663, is an oral COX-2 inhibitor that is selective. Its IC50 values for COX-2, COX-1, and pure human COX-2 in human whole blood are 1.1 μM, 116 μM, and 5, respectively. I.Q. PGE2 produced by CHO (COX-2) cells (IC50, 79 nM), detergent-pure human COX-2 (IC50, 4.1 μM), and purified PGE2 produced by U937 microsomes Effect (low substrate; IC50, 12.1 μM) are all inhibited by etoricoxib (MK-0663). On the other hand, etoricoxib (MK-0663) has a low Ki of 167 μM and minimal action against COX-1 [1].
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ln Vivo |
In rats, carrageenan-induced paw edema, carrageenan-induced paw pain hypersensitivity, and endotoxin-induced fever are all dose-dependently inhibited by etoricoxib (MK-0663) (0.1-30 mg/kg, po). In a rat hyperalgesia model, etoricoxib (≥10 mg/kg) totally reverses the hyperalgesic response. Rats' urine excretion of 51Cr is unaffected by etoricoxib (MK-0663) at 200 mg/kg/day, and monkeys are unaffected by 100 mg/kg/day of the drug [1]. Rats' levels of glutathione Peptide reductase (GSHRd) and total glutathione (tGSH) are effectively decreased whereas those of malondialdehyde (MDA) and myeloperoxidase (MPO) are effectively increased by etoricoxib (MK-0663) at 50 and 100 mg/kg. Rats' NO decrease is considerably inhibited by etoricoxib (MK-0663) at a dose of 100 mg/kg [2]. Rats with 1,2-dimethylhydrazine dihydrochloride (DMH)-induced numerous plaque lesions, hyperplasia, and dysplasia can benefit from etoricoxib (MK-0663) (0.64 mg/kg, po) [3].
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References |
[1]. Riendeau D, et al.Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2. J Pharmacol Exp Ther. 2001 Feb;296(2):558-66.
[2]. Kunak CS, et al. The Effect of Etoricoxib on Hepatic Ischemia-Reperfusion Injury in Rats. Oxid Med Cell Longev. 2015;2015:598162. [3]. Tanwar L, et al. Anti-proliferative and apoptotic effects of etoricoxib, a selective COX-2 inhibitor, on 1,2-dimethylhydrazine dihydrochloride-induced colon carcinogenesis. Asian Pac J Cancer Prev. 2010;11(5):1329-33 |
Molecular Formula |
C18H15N2O2SCL
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Molecular Weight |
358.8419
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CAS # |
202409-33-4
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Related CAS # |
Etoricoxib-d4;1131345-14-6;Etoricoxib-13C,d3;2748267-73-2;Etoricoxib-d3;850896-71-8
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SMILES |
O=S(C1=CC=C(C2=CC(Cl)=CN=C2C3=CC=C(C)N=C3)C=C1)(C)=O
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InChi Key |
MNJVRJDLRVPLFE-UHFFFAOYSA-N
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InChi Code |
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
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Chemical Name |
5-Chloro-6'-methyl-3-[4-(methylsulfonyl)phenyl]-2,3'-bipyridine
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Synonyms |
L-791456, L791456, L 791456, MK-0663, MK 0663, MK0663; Arcoxia
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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 : ~100 mg/mL (~278.68 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.97 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.97 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.97 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 | 2.7868 mL | 13.9338 mL | 27.8676 mL | |
5 mM | 0.5574 mL | 2.7868 mL | 5.5735 mL | |
10 mM | 0.2787 mL | 1.3934 mL | 2.7868 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.