CRTH2-IN-1

CRTH2-IN-1 (Ramatroban analog, Compound 5) is a novel prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC₅₀ of 7 nM in a human whole blood eosinophil shape change assay (hESC). CRTH2-IN-1 (Ramatroban analog) is a novel tricyclic antagonist of the prostaglandin D2 receptor DP2 (CRTH2) with efficacy in a murine model of allergic rhinitis. Human prostaglandin D1 receptor (hDP1) binding is performed using ³H-PGD2 and human platelet membranes. Human thromboxane receptor (hTP) binding performed using human platelet membranes and ³H-SQ-29,548. Human prostacyclin receptor (hIP) binding perfomed using hIP/293 membranes and ³Hiloprost. CRTH2-IN-1 inhibits hDP1 binding with an IC₅₀ of 1μM. CRTH2-IN-1 inhibits hTP and hIP binding with IC₅₀s of >100 μM. CRTH2-IN-1 inhibits human CYP isoforms CYP3A4, CYP 2C9 and CYP2D6 with IC₅₀s of 7, 5 and >30 μM, respectively^[1].

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