Mofezolac
Names
Biological Activity
[Description]:
Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities[1].
[Related Catalog]:
[Target]
COX-1:1.44 nM (IC50)
COX-2:447 nM (IC50)
[In Vitro]
Mofezolac inhibits platelet aggregation with an IC50 of 0.45 μM in human platelet rich plasma (hPRP) assay[2]. Mofezolac slightly increase Bortezomib cytotoxic effect on multiple myeloma (MM) cell lines (NCI-H929 and RPMI-8226) and affects MM cell cycle and apoptosis when co-administered with the proteasome inhibitor Bortezomib[2].
[In Vivo]
Mofezolac (1-30 mg/kg; oral administration; once) treatment results in the suppression of writhing induced by the intraperitoneal injection of phenyl-p-benzoquinone in mice[1]. Animal Model: Female ddY mice (4 week old, 18-27 g) injected with phenyl-p-benzoquinone (PQ)[1] Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Oral administration; once Result: Dose-dependently suppressed the writhing induced by PQinjection in mice.
[References]
Chemical & Physical Properties
[ Density]:
1.25g/cm3
[ Boiling Point ]:
527.2ºC at 760 mmHg
[ Molecular Formula ]:
C19H17NO5
[ Molecular Weight ]:
339.34200
[ Flash Point ]:
272.7ºC
[ Exact Mass ]:
339.11100
[ PSA ]:
81.79000
[ LogP ]:
3.65290
[ Index of Refraction ]:
1.579
[ Storage condition ]:
-20℃
Toxicological Information
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- NY2101000
- CHEMICAL NAME :
- 5-Isoxazoleacetic acid, 3,4-bis(4-methoxyphenyl)-
- CAS REGISTRY NUMBER :
- 78967-07-4
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 13
- MOLECULAR FORMULA :
- C19-H17-N-O5
- MOLECULAR WEIGHT :
- 339.37
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 887 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 342 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 510 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Behavioral - coma Behavioral - antipsychotic
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 1528 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Behavioral - coma Behavioral - antipsychotic
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 275 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Behavioral - coma Behavioral - antipsychotic
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 545 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 800 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 18200 mg/kg/91D-I
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - other changes in urine composition Endocrine - changes in spleen weight Nutritional and Gross Metabolic - changes in chlorine
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 1820 mg/kg/91D-I
- TOXIC EFFECTS :
- Gastrointestinal - peritonitis Endocrine - changes in thymus weight Blood - changes in erythrocyte (RBC) count
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 1650 mg/kg
- SEX/DURATION :
- female 7-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 2600 mg/kg
- SEX/DURATION :
- female 17-21 day(s) after conception lactating female 21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - parturition Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Newborn - stillbirth
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 2600 mg/kg
- SEX/DURATION :
- female 6-18 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death
MUTATION DATA
- TYPE OF TEST :
- Cytogenetic analysis
- TEST SYSTEM :
- Rodent - hamster Lung
- DOSE/DURATION :
- 600 mg/L
- REFERENCE :
- JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 2),239,1990