1. Immunology/Inflammation
  2. COX
  3. Etoricoxib

Etoricoxib (Synonyms: MK-0663; L-791456)

Cat. No.: HY-15321 Purity: 99.10%
Handling Instructions

Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.

For research use only. We do not sell to patients.

Etoricoxib Chemical Structure

Etoricoxib Chemical Structure

CAS No. : 202409-33-4

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10 mM * 1 mL in DMSO USD 66 In-stock
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10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 120 In-stock
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100 mg USD 192 In-stock
Estimated Time of Arrival: December 31
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Description

Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.

IC50 & Target

COX-2

1.1 μM (IC50, in human whole blood)

COX-1

116 μM (IC50, in human whole blood)

In Vitro

Etoricoxib (MK-0663) is a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM, 116 μM and 5 μM for COX-2, COX-1 in human whole blood and purified human COX-2, respectively. Etoricoxib (MK-0663) shows inhibitory effect on PGE2 production by CHO (COX-2) cells (IC50, 79 nM), on purified human COX-2 with detergent (IC50, 4.1 μM), and on purified PGE2 production by U937 microsomes (low substrate; IC50, 12.1 μM). However, Etoricoxib (MK-0663) has little activity against COX-1 with a Ki of 167 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Etoricoxib (MK-0663) (0.1-30 mg/kg, p.o.) dose-dependently inhibits carrageenan-induced paw edema, carrageenan-induced paw hyperalgesia, and endotoxin-induced pyresis in rats. Etoricoxib (≥10 mg/kg) completely reverses hyperalgesia response in the rat hyperalgesia model. Etoricoxib (MK-0663) (200 mg/kg/day) has no effect on urinary 51Cr excretion in rats, and nor in monkeys at 100 mg/kg/day[1]. Etoricoxib (MK-0663) (50 and 100 mg/kg) potently increases the malondialdehyde (MDA) and myeloperoxidase (MPO) levels, and decreases the total glutathione (tGSH) and glutathione reductase (GSHRd) levels in rats. Etoricoxib (MK-0663) (100 mg/kg) significantly inhibits the decrease of NO in rats[2]. Etoricoxib (MK-0663) (0.64 mg/kg, p.o.) reduces the features such as multiple plaque lesions, hyperplasia and dysplasia induced by 1,2-dimethylhydrazine dihydrochloride (DMH) in rats[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

358.84

Formula

C₁₈H₁₅ClN₂O₂S

CAS No.

202409-33-4

SMILES

O=S(C1=CC=C(C2=CC(Cl)=CN=C2C3=CC=C(C)N=C3)C=C1)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (278.68 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.97 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.97 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.97 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[3]

Rats[3]
Animals are assorted into the following groups with four to six animals in each group: Control Group, Animals are administrated the vehicle (1mM EDTA-saline subcutaneously) in weekly injection and 0.5% carboxymethyl cellulose per oral daily; 1,2-dimethylhydrazine dihydrochloride (DMH) Group, animals are administrated with DMH weekly at a dose of 30 mg/kg body weight subcutaneously, DMH is freshly prepared in 1mM EDTA-saline, pH adjusted to 7.0 using dilute NaOH solution; DMH + Etoricoxib Group, Etoricoxib (MK-0663) is given daily per oral at its therapeutic anti-inflammatory dose (ED50 for rats, 0.64 mg/kg body weight) to the animals along with the weekly administration of DMH; and Etoricoxib Group: Etoricoxib (MK-0663) alone is administered orally daily (0.64 mg/kg body weight). After six weeks, animals are kept on overnight fasting with drinking water ad libitum and sacrificed the next day. The animal body weights in all the groups are recorded once in a week till the termination.[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

EtoricoxibMK-0663 L-791456MK0663MK 0663L791456L 791456L-791456COXCyclooxygenaseInhibitorinhibitorinhibit

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Etoricoxib
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