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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 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
|Related Prostaglandin Receptor Products|
Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist.
Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
|MK-2894 sodium salt
MK-2894 sodium salt is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM).
Furprofen is an non-steroidal anti-inflammatory drug (NSAID) with analgesic properties. Furprofen acts via the inhibition of prostaglandin (PGE) synthesis. Furprofen can be treated orally for the relief of pain.
MK-2894 IS AN EFFECTIVE, SELECTIVE, HIGH-AFFINITY (Ki=0.56 nM) of prostaglandin receptor 4 (EP4 receptor) antagonists (IC50=2.5 nM)。 MK-2894 has strong anti-inflammatory activity in animal pain/inflammation models and can be used in arthritis studies.
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