Biologically Active Small Molecules

A selective PPARd agonist that acts as a partial agonist (EC50 = 53 nM) in transactivation assays and as a full agonist (EC50 = 30 nM) in the oxidation of free fatty acid increases HDL levels, decreases LDL and TG levels, and improves insulin

A potent PLD2 inhibitor, both in vitro (IC₅₀ = 140 nM) and in cells (IC₅₀ = 110 nM) also effective as a PLD1 inhibitor at higher concentrations (IC₅₀ = 5.1 &muM in vitro, 1.

A potent PLD2 inhibitor, both in vitro (IC₅₀ = 140 nM) and in cells (IC₅₀ = 110 nM) also effective as a PLD1 inhibitor at higher concentrations (IC₅₀ = 5.1 &muM in vitro, 1.

A potent PLD2 inhibitor, both in vitro (IC₅₀ = 140 nM) and in cells (IC₅₀ = 110 nM) also effective as a PLD1 inhibitor at higher concentrations (IC₅₀ = 5.1 &muM in vitro, 1.

A potent PLD2 inhibitor, both in vitro (IC₅₀ = 140 nM) and in cells (IC₅₀ = 110 nM) also effective as a PLD1 inhibitor at higher concentrations (IC₅₀ = 5.1 &muM in vitro, 1.

A potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 10 nM R enantiomer of CAY10595 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 7.3 nM.

A potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 10 nM R enantiomer of CAY10595 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 7.3 nM.

A potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 10 nM R enantiomer of CAY10595 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 7.3 nM.

A potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 40 nM.

A potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 40 nM.

A potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 40 nM.

A very potent agonist of EP4, binding with a Ki value of 1.2 nM does not bind EP1, EP2, EP3, DP, FP, IP, or TP receptors.