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Indomethacin farnesil

Cat. No. M30710
Indomethacin farnesil Structure
Synonym:

Indometacin farnesil

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Quality Control & Documentation
Biological Activity

Indomethacin farnesil is an orally active proagent of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.

Chemical Information
Molecular Weight 562.14
Formula C34H40ClNO4
CAS Number 85801-02-1
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] K Nomura, et al. Br J Dermatol. Angiolymphoid hyperplasia with eosinophilia: successful treatment with indomethacin farnesil

[2] S Hirohata, et al. Nihon Rinsho Meneki Gakkai Kaishi. Interaction of indometacin farnesil, a new nonsteroidal antiinflammatory drug with peripheral blood mononuclear cells from patients with rheumatoid arthritis

[3] T Arakawa, et al. Drugs Exp Clin Res. Ulcerogenicity and effect on inhibition of prostaglandin generation of indometacin farnesil, a prodrug of indomethacin, in rat gastric mucosa: comparison with indomethacin or loxoprofen

[4] S Kumakura, et al. Agents Actions. Inhibitory effect of indomethacin farnesil, a novel antiinflammatory prodrug, on carrageenin-induced inflammation in rats

[5] M Mishima, et al. Xenobiotica. Metabolic fate of indometacin farnesil, a prodrug of indomethacin: characteristic biotransformation of indometacin farnesil in rats

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Keywords: Indomethacin farnesil, Indometacin farnesil supplier, COX, inhibitors, activators


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