Description
MK-2894 is a highly potent and selective inhibitor of EP4 receptor with IC50 value of 2.5 nM.
Product Overview
MK-2894 is a highly potent and selective inhibitor of EP4 receptor with IC50 value of 2.5 nM. MK-2894 is a highly selective and potent second generation EP4 antagonist with a Ki of 0.56±0.1nM in the radio ligand binding assay using membranes prepared from human EP1-4 overexpressed HEK 293 cell lines. And the EP4 functional assay measures the inhibition of PGE2-induced cAMP accumulation with IC50 of 2.5±0.7nM. In the AIA model and GI tolerability model in male SD rats, MK-2894 shows a dose-dependent inhibition of pain response with ED50 of 0.36 mg/kg. It also has the potent activity in inhibiting chronic pawswelling with ED50 of 0.02 mg/kg/day. Overall, MK-2894 displays the desired potency, selectivity, pharmacokinetic, and GI tolerability profile for further development and represents a potential safer alternative for treating pain and inflammation than traditional NSAIDs and coxibs.
IC50
2.5 nM (Ki=0.56±0.1 nM）;
Molecular Formula
C25H22F3NO3S
Chemical Name
4-[1-[[2,5-dimethyl-4-[[4-(trifluoromethyl)phenyl]methyl]thiophene-3-carbonyl]amino]cyclopropyl]benzoic acid
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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