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      Timapiprant (OC000459)
      Timapiprant (OC000459)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V1807
      CAS #: 851723-84-7 Purity ≥98%

      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)

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      Molecular Weight (MW)348.37
      FormulaC21H17FN2O2
      CAS No.851723-84-7, 950688-14-9 (sodium salt)
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 4 mg/mL (11.5 mM)
      Water: <1 mg/mL
      Ethanol:<1 mg/mL
      Other info
      		Chemical Name: 2-(5-fluoro-2-methyl-3-(quinolin-2-ylmethyl)-1H-indol-1-yl)acetic acid

      SMILES Code: O=C(O)CN1C(C)=C(CC2=NC3=CC=CC=C3C=C2)C4=C1C=CC(F)=C4 

      Exact Mass: 348.1274 

      SynonymsOC000459; OC-000459; OC 000459


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      In Vitro

      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.

      In VivoOC000459 administrated at doses of 2 mg/kg p.o. in the Sprague-Dawley rats shows plasma half-life of 2.9 hours, time that maximal plasma concentration is achieved of 1.3 hours, maximal plasma concentration achieved is 1.54 μg/mL. OC000459 orally administrated 0.5 hour before injection of DK-PGD2 leads to a dose-dependent reduction in blood eosinophilia with ED50 of 0.04 mg/kg in rats. OC000459 orally administrated 0.5 hour before injection of DK-PGD2 also leads to a dose-dependent inhibition eosinophil accumulation ED50 of 0.01 mg/kg in rats. OC000459 (200 mg twice daily for 28 days) administrated in patients with moderate persistent asthma shows improvement in quality of life as analysed for both the Full Analysis (FA) population and the Per Protocol (PP) population. In those patients, OC000459 improves the night-time symptom scores, reduces the geometric mean sputum eosinophil count and respiratory infections. OC000459 (200 mg twice daily) treatment inhibits the later asthmatic responses and the post allergen increase in sputum eosinophils in steroid naive asthmatic patients.
      Animal modelSprague-Dawley rats 
      Formulation & DosageDissolved in 10% DMSO/saline solution; 10 mg/kg; Oral administration
      ReferencesJ Pharmacol Exp Ther. 2012 Feb;340(2):473-82.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

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