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MF-766

Cat. No. M10857
MF-766  Structure
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Biological Activity

MF-766 is a highly effective, selective and orally active EP4 antagonist.Ki The value is 0.23 nM. MF-766 behaves as a complete antagonist with its IC in functional detection50 1.4 nM (becomes 1.8 nM when 10% HS is present). MF-766 can be used for cancer and inflammatory disease research.

Chemical Information
Molecular Weight 478.46
Formula C27H21F3N2O3
CAS Number 1050656-06-8
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] Yun Wang, et al. Oncoimmunology. Combination of EP 4 antagonist MF-766 and anti-PD-1 promotes anti-tumor efficacy by modulating both lymphocytes and myeloid cells

[2] John Colucci, et al. Bioorg Med Chem Lett. Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain

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