MOFEZOLAC

Details

Stereochemistry	ACHIRAL
Molecular Formula	C19H17NO5
Molecular Weight	339.342
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=CC=C(C=C1)C2=NOC(CC(O)=O)=C2C3=CC=C(OC)C=C3

InChI

InChIKey=DJEIHHYCDCTAAH-UHFFFAOYSA-N

InChI=1S/C19H17NO5/c1-23-14-7-3-12(4-8-14)18-16(11-17(21)22)25-20-19(18)13-5-9-15(24-2)10-6-13/h3-10H,11H2,1-2H3,(H,21,22)

HIDE SMILES / InChI

Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/16473424
Curator's Comment: description was created based on several sources, including

Mofezolac is an NSAID ) (non-steroidal anti-inflammatory drug), which acts via the cyclooxygenase enzyme, preferentially to COX-1. It also has potent inhibitory activity on the algesic responses induced by the mechanical stimulus of the inflamed tissue. It was introduced for the treatment of postoperative and posttraumatic pain, acute upper respiratory tract pain, osteoarthritis, and lumbago. It marketed only in Japan by Yoshitomi Pharmaceutical Ltd. Japan, was approved in July 1994.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Cyclooxygenase-1 131 Target ID: CHEMBL221 Sources: http://www.ncbi.nlm.nih.gov/pubmed/9777656	Inhibitor 8504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Scapulohumeral periarthritis 3 Sources: https://www.mimaki-family-japan.com/item/detail?item_prefix=TF&item_code=004288&item_branch=001	Primary		Not Provided 511	Disopain Approved Use used to relieve inflammation/pain of lower back, cervicobrachial syndrome and scapulohumeral periarthritis. It is also used to relieve inflammation/pain after operation, trauma or tooth extraction. Launch Date 1994
Cervicobrachial syndrome 1 Sources: https://www.mimaki-family-japan.com/item/detail?item_prefix=TF&item_code=004288&item_branch=001	Primary		Not Provided 511	Disopain Approved Use used to relieve inflammation/pain of lower back, cervicobrachial syndrome and scapulohumeral periarthritis. It is also used to relieve inflammation/pain after operation, trauma or tooth extraction. Launch Date 1994

PubMed

Title	Date	PubMed
Drug-target interaction prediction from chemical, genomic and pharmacological data in an integrated framework.	2010-06-15	20529913
The effect of selective cyclooxygenase-2 inhibitor on human osteoclast precursors to influence osteoclastogenesis in vitro.	2009	19198759
Role of interleukin-1beta and tumor necrosis factor-alpha-dependent expression of cyclooxygenase-2 mRNA in thermal hyperalgesia induced by chronic inflammation in mice.	2008-03-18	18262365
Suppression of azoxymethane-induced colon cancer development in rats by a cyclooxygenase-1 selective inhibitor, mofezolac.	2006-10	16984374
Zaltoprofen, a non-steroidal anti-inflammatory drug, inhibits bradykinin-induced pain responses without blocking bradykinin receptors.	2006-04	16473424
Significance of cyclooxygenase-2 induced via p38 mitogen-activated protein kinase in mechanical stimulus-induced peritoneal adhesion in mice.	2005-04	15576468
Induction of cyclooxygenase-1 in cultured synovial cells isolated from rheumatoid arthritis patients.	2004-06	15167967
Combined effects of cyclooxygenase-1 and cyclooxygenase-2 selective inhibitors on intestinal tumorigenesis in adenomatous polyposis coli gene knockout mice.	2004-04-20	14991580
Constitutive expression and involvement of cyclooxygenase-2 in human megakaryocytopoiesis.	2004-03	14726416
COX-2/VEGF-dependent facilitation of tumor-associated angiogenesis and tumor growth in vivo.	2003-10	14563940
Role of kinin and prostaglandin in cutaneous thermal nociception.	2002-12	12489814
Cyclooxygenase-2 inhibitors attenuate increased blood pressure in renovascular hypertensive models, but not in deoxycorticosterone-salt hypertension.	2002-11	12484518
Inhibitory effects of mofezolac, a cyclooxygenase-1 selective inhibitor, on intestinal carcinogenesis.	2002-09	12189188
Participation of cyclooxygenases in cutaneous thermal nociception under non-inflamed and inflamed conditions.	2001-05	11409492

Patents

Sample Use Guides

In Vivo Use Guide

General dosage regimen (for adults): Take 1 tablet (75mg of the active ingredient) at a time three times a day after meals.

Route of Administration: Oral

In Vitro Use Guide

Mofezolac affected neither the number of TRAP-positive multinucleated cells nor the extent of lacunar resorption pits.

Name

Type

Language

MOFEZOLAC [JAN]

Preferred Name

English

MOFEZOLAC

Official Name

English

MOFEZOLAC [MI]

Common Name

English

3,4-BIS(P-METHOXYPHENYL)-5-ISOXAZOLEACETIC ACID

Common Name

English

MOFEZOLAC [MART.]

Common Name

English

mofezolac [INN]

Common Name

English

Mofezolac [WHO-DD]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C257