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Mofezolac

Cat. No. M30613
Mofezolac Structure
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 339.34
Formula C19H17NO5
CAS Number 78967-07-4
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Miroslav Sisa, et al. Arch Pharm (Weinheim). SC-560 and mofezolac isosteres as new potent COX-1 selective inhibitors with antiplatelet effect

[2] Maria Grazia Perrone, et al. Eur J Med Chem. An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid

[3] Maria Grazia Perrone, et al. Eur J Med Chem. Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier

[4] M Takemoto, et al. J Toxicol Sci. [Antigenicity test of mofezolac (N-22)]

[5] N Ono, et al. Nihon Yakurigaku Zasshi. [Pharmacological profile of mofezolac, a new non-steroidal analgesic anti-inflammatory drug]

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