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Chemical Structure : OC000459
CAS No.: 851723-84-7
Catalog No.: PC-38844Not For Human Use, Lab Use Only.
OC000459 is a potent, selective, and orally active D prostanoid receptor 2 (DP2, CRTH2) antagonist with Ki of 13/3 nM for human/recombinant DP2, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $88 | In stock | |
| 25 mg | $138 | In stock | |
| 50 mg | $228 | In stock | |
| 100 mg | Get quote |
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OC000459 (Timapiprant) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, CRTH2) antagonist with Ki of 13/3 nM for human/recombinant DP2, respectively.
OC000459 does not interfere with the ligand binding properties or functional activities of other prostanoid receptors (prostaglandin E1-4 receptors, D1, thromboxane receptor, prostacyclin receptor, and prostaglandin F receptor).
OC000459 inhibited chemotaxis (IC50= 28 nM) of human Th2 lymphocytes and cytokine production (IC50=19 nM) by human Th2 lymphocytes.
OC000459 competitively antagonized eosinophil shape change responses induced by PGD₂ in both isolated human leukocytes (pK(B)=7.9) and human whole blood (pK(B)=7.5) but did not inhibit responses to eotaxin, 5-oxo-eicosatetraenoic acid, or complement component C5a.
OC000459 is orally bioavailable in rats and effective in inhibiting blood eosinophilia induced by 13,14-dihydro-15-keto-PGD₂ (DK-PGD₂) with ED50 of 0.04 mg/kg (p.o.) and airway eosinophilia in response to an aerosol of DK-PGD₂ in guinea pigs (ED50=0.01 mg/kg p.o.).
| M.Wt | 348.377 | |
| Formula | C21H17FN2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
5-fluoro-2-methyl-3-(2-quinolinylmethyl)-1H-indole-1-acetic acid |
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1. Pettipher R, et al. J Pharmacol Exp Ther. 2012 Feb;340(2):473-82.
2. Barnes N, et al. Clin Exp Allergy. 2012 Jan;42(1):38-48.
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