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CRTH2-IN-1 (Ramatroban analog) (Synonyms: Ramatroban analog)

Catalog No.GC31998

CRTH2-IN-1 (analogue de Ramatroban) (analogue de Ramatroban) est un antagoniste sélectif du récepteur de la prostaglandine D2 DP2 (CRTH2) avec une IC50 de 6 nM dans un test de liaison de DP2 humain.

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CRTH2-IN-1 (Ramatroban analog) Chemical Structure

Cas No.: 926661-54-3

Taille Prix Stock Qté
5mg
321,00 $US
En stock
10mg
552,00 $US
En stock
25mg
1 103,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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].

[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.

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