Technical Data
| Formula | C21H17FN2O2 |
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| Molecular Weight | 348.37 | CAS No. | 851723-84-7 | ||||
| Solubility (25°C)* | In vitro | DMSO | 4 mg/mL (11.48 mM) | ||||
| Water | Insoluble | ||||||
| Ethanol | Insoluble | ||||||
| In Vivo (Add solvents to the product individually and in order.) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2. | ||
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| In vitro | OC000459 inhibits the binding of [3H]PGD2 to membranes from CHO cells transfected with human DP2 with Ki of 13 nM. This compound also displaces [3H]PGD2 from membranes from human Th2 lymphocytes with Ki of 4 nM. It antagonises PGD2-mediated calcium mobilisation in a concentration-dependent manner with IC50 of 28 nM in intact CHO cells expressing DP2. This chemical inhibits chemotaxis of human Th2 cells in response to PGD2 (10 nM) with IC50 of 28 nM. It antagonises the effect of PGD2 competitively in both the isolated leukocyte preparation and heparinised human whole blood. This compound inhibits eosinophil shape change responses to DK-PGD2 with IC50 of 11 nM. It inhibits the activation of Th2 cells and eosinophils in response to mast cell supernatants. | ||
| In Vivo | OC000459 administered at doses of 2 mg/kg p.o. in Sprague-Dawley rats shows a 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. This compound orally administered 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. It orally administered 0.5 hour before injection of DK-PGD2 also leads to a dose-dependent inhibition of eosinophil accumulation with ED50 of 0.01 mg/kg in rats. This chemical (200 mg twice daily for 28 days) administered 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, it improves the night-time symptom scores, reduces the geometric mean sputum eosinophil count and respiratory infections. This compound (200 mg twice daily) treatment inhibits the later asthmatic responses and the post allergen increase in sputum eosinophils in steroid naive asthmatic patients. |
Protocol (from reference)
| Animal Study:[1] |
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References
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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