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FR122047 

Cat. No. M28145
FR122047  Structure
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Quality Control & Documentation
Biological Activity

FR122047 (hydrochloride) is a selective and oral active inhibitor of COX-1 with an IC50 of 28 nM. FR122047 hydrochloride has antiplatelet, analgesic and anti-inflammatory effects in vivo.

Chemical Information
Molecular Weight 459.99
Formula C23H26ClN3O3S
CAS Number 130717-51-0
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] Hyo-Soon Jeong, et al. Oncol Rep. Induction of cell growth arrest and apoptotic cell death in human breast cancer MCF-7 cells by the COX-1 inhibitor FR122047

[2] Tomohiro Abe, et al. Ophthalmic Res. Effects of intravenous administration of FR122047 (a selective cyclooxygenase 1 inhibitor) and FR188582 (a selective cyclooxygenase 2 inhibitor) on prostaglandin-E2-induced aqueous flare elevation in pigmented rabbits

[3] Takehiro Ochi, et al. Br J Pharmacol. Differential effect of FR122047, a selective cyclo-oxygenase-1 inhibitor, in rat chronic models of arthritis

[4] T Ochi, et al. Eur J Pharmacol. The analgesic effect profile of FR122047, a selective cyclooxygenase-1 inhibitor, in chemical nociceptive models

[5] M Dohi, et al. Eur J Pharmacol. The anti-platelet actions of FR122047, a novel cyclooxygenase inhibitor

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Keywords: FR122047  supplier, COX, inhibitors, activators


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