CRTH2-IN-1  (Synonyms: Ramatroban analog)

CRTH2-IN-1 (Ramatroban analog) is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC₅₀ of 6 nM in a human DP2 binding assay.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

416.47

C₂₁H₂₁FN₂O₄S

926661-54-3

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• [1]. Stearns BA, et al. Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine modelof allergic rhinitis. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51.  [Content Brief]