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Description: Timapiprant (formerly known as OC000459; OC-000459) is a novel, potent, selective, and orally bioactive prostanoid receptor 2 (DP2- also known as CRTH2)) antagonist with IC50 of 13 nM. It reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen, a randomised, placebo-controlled, double-blind trial. OC000459 inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. As an antagonist of DP2, OC000459 can prevent PGD2 from binding to human DP2 and rat recombinant DP2 with Ki values of 4nM and 3nM. OC000459 treatment inhibited LAR and post-allergen increase in sputum eosinophils. OC000459 appears to inhibit allergic inflammation in asthma.
References: J Pharmacol Exp Ther. 2012 Feb;340(2):473-82.
Related CAS #: 950688-14-9 (sodium salt); 51723-84-7 (free acid)
Product Catalog 2022
Guide to Product Handling
SMILES Code: O=C(O)CN1C(C)=C(CC2=NC3=CC=CC=C3C=C2)C4=C1C=CC(F)=C4
Exact Mass: 348.1274
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: OC000459 inhibits the binding of [3H]PGD2 to membranes from CHO cells transfected with human DP2 with Ki of 13 nM. OC000459 also displaces [3H]PGD2 from membranes from human Th2 lymphocytes with Ki of 4 nM. OC000459 antagonizes PGD2-mediated calcium mobilization in a concentration-dependent manner with IC50 of 28 nM in intact CHO cells expressing DP2. OC000459 inhibits chemotaxis of human Th2 cells in response to PGD2 (10 nM) with IC50 of 28 nM. OC000459 (< 3 μM) antagonizes the effect of PGD2 competitively in both the isolated leukocyte preparation and heparinized human whole blood. OC000459 inhibits eosinophil shape change responses to DK-PGD2 with IC50 of 11 nM. OC000459 (1 μM) inhibits the activation of Th2 cells and eosinophils in response to mast cell supernatants.
Cell Assay: Timapiprant (OC000459) (0.0001 μM-10 μM; 5 hours) inhibits chemotaxis (IC50=0.028 μM) of human Th2 lymphocytes and cytokine production (IC50=0.019 μM) by human Th2 lymphocytes. Timapiprant (OC000459) (1 μM) inhibits the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells.
Lot#: V180701,Purity ≥98%
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MSDS
NMR
HPLC
Lot#: V180702,Purity ≥98%