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EP3 antagonist 4

Cat. No. M41910
EP3 antagonist 4 Structure
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Biological Activity

EP3 antagonist 4 is an EP3 antagonist, with a Ki value of 2 nM for hEP.

Chemical Information
Molecular Weight 577.91
Formula C22H20Cl3FN4O3S2
CAS Number 2408297-80-1
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] Georg A Petroianu. Int J Mol Sci. Hyperthermia and Serotonin: The Quest for a "Better Cyproheptadine"

[2] Ryan P Ceddia et al. Prostaglandins Other Lipid Mediat. The effect of the EP3 antagonist DG-041 on male mice with diet-induced obesity

[3] Kazuhiko Mizukami et al. Naunyn Schmiedebergs Arch Pharmacol. Pharmacological properties of ASP7657, a novel, potent, and selective prostaglandin EP4 receptor antagonist

[4] Marie-Anne Mawhin et al. Prostaglandins Other Lipid Mediat. The receptor EP3 to PGE2: A rational target to prevent atherothrombosis without inducing bleeding

[5] Kohichi Kawahara et al. Biochim Biophys Acta. Prostaglandin E2-induced inflammation: Relevance of prostaglandin E receptors

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