Art. -Nr.: HY-15321

Etoricoxib

(Synonyms: MK-0663; L-791456)

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

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Reinheit: 99.91%
CAS. Nr.: 202409-33-4
Formel: C₁₈H₁₅ClN₂O₂S
Molecular Weight:358.84

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Etoricoxib Chemical Structure

CAS. Nr.: 202409-33-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

COX-2

1.1 μM (IC₅₀, in human whole blood)

COX-1

116 μM (IC₅₀, in human whole blood)

Alle COX Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.081 μM Compound: 28	Inhibition of human COX-2 transfected in CHO cells using arachidonic acid as substrate Inhibition of human COX-2 transfected in CHO cells using arachidonic acid as substrate	[PMID: 30396033]
CHO	IC₅₀	0.081 μM Compound: 33	In vitro inhibition of PGE-2 produced by arachidonic acid-stimulated CHO cells stably expressing human Prostaglandin G/H synthase 2 In vitro inhibition of PGE-2 produced by arachidonic acid-stimulated CHO cells stably expressing human Prostaglandin G/H synthase 2	[PMID: 9873621]
U-937	IC₅₀	12 μM Compound: 33	Inhibition of Prostaglandin G/H synthase 1 was measured by the inhibition of PGE-2 produced by microsomes from U937 cells at subsaturating arachidonic acid conc. Inhibition of Prostaglandin G/H synthase 1 was measured by the inhibition of PGE-2 produced by microsomes from U937 cells at subsaturating arachidonic acid conc.	[PMID: 9873621]

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 K_i of 167 μM^[1].

MedChemExpress (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].
Etoricoxib can cross the blood-brain barrier very quickly^[4].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 202409-33-4
Appearance Solid
Molecular Weight 358.84
Formel C₁₈H₁₅ClN₂O₂S
Color Light yellow to yellow
SMILES

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

MK-0663; L-791456
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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bioRxiv

A drug repurposing screen reveals dopamine signaling as a candidate therapeutic pathway for PIGA-CDG. [Abstract]

2026 Apr 18:2026.04.17.719256. PMID: 42039650

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (278.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[2]. Kunak CS, et al. The Effect of Etoricoxib on Hepatic Ischemia-Reperfusion Injury in Rats. Oxid Med Cell Longev. 2015;2015:598162. [Content Brief]

[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. [Content Brief]

[4]. Piirainen A, et al. The Cerebrospinal Fluid Distribution of Postoperatively Administred Dexketoprofen and Etoricoxib and Their Effect on Pain and Inflammatory Markers in Patients Undergoing Hip Arthroplasty. Clin Drug Investig. 2016 Jul;36(7):545-55. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7868 mL	13.9338 mL	27.8676 mL	69.6689 mL
	5 mM	0.5574 mL	2.7868 mL	5.5735 mL	13.9338 mL
	10 mM	0.2787 mL	1.3934 mL	2.7868 mL	6.9669 mL
	15 mM	0.1858 mL	0.9289 mL	1.8578 mL	4.6446 mL
	20 mM	0.1393 mL	0.6967 mL	1.3934 mL	3.4834 mL
	25 mM	0.1115 mL	0.5574 mL	1.1147 mL	2.7868 mL
	30 mM	0.0929 mL	0.4645 mL	0.9289 mL	2.3223 mL
	40 mM	0.0697 mL	0.3483 mL	0.6967 mL	1.7417 mL
	50 mM	0.0557 mL	0.2787 mL	0.5574 mL	1.3934 mL
	60 mM	0.0464 mL	0.2322 mL	0.4645 mL	1.1611 mL
	80 mM	0.0348 mL	0.1742 mL	0.3483 mL	0.8709 mL
	100 mM	0.0279 mL	0.1393 mL	0.2787 mL	0.6967 mL

Keywords

Etoricoxib

1 Cited Publications

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Etoricoxib

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Publications Citing Use of MedChemExpress (MCE) Etoricoxib

Alle COX Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Etoricoxib Related Classifications

HY-15321 Related Classifications