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Isoxepac

Cat. No. M30295
Isoxepac Structure
Synonym:

HP 549

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Biological Activity

Isoxepac (HP 549) is a nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory, analgesic and antipyretic activity. Isoxepac has been studied in rat, rabbit, dog, rhesus monkey, etc.

Chemical Information
Molecular Weight 268.26
Formula C16H12O4
CAS Number 55453-87-7
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] W J Honig, et al. J Clin Pharmacol. Analgesic effect of isoxepac on postmeniscectomy pain: a controlled trial

[2] J Scott, et al. Rheumatol Rehabil. Analgesic action of isoxepac

[3] L B Svendsen, et al. Scand J Rheumatol. A comparison of the effects of HP 549 (Isoxepac), indomethacin and acetylsalicylic acid (Aspirin) on gastric mucosa in man

[4] L S Gerlis, et al. Rheumatol Rehabil. Isoxepac in rheumatoid arthritis: a double-blind comparison with aspirin

[5] H P Illing, et al. Drug Metab Dispos. Species differences in the disposition and metabolism of 6,11-dihydro-11-oxodibenz[be]oxepin-2-acetic acid (isoxepac) in rat, rabbit, dog, rhesus monkey, and man

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