OC000459

Catalog No.S2822

OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2.

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OC000459 Chemical Structure

OC000459 Chemical Structure
Molecular Weight: 348.37

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2.
Targets DP2 [1]
IC50 13 nM
In vitro 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. [1]
In vivo OC000459 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. [1] 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. [2] OC000459 (200 mg twice daily) treatment inhibits the later asthmatic responses and the post allergen increase in sputum eosinophils in steroid naive asthmatic patients. [3]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Ligand Binding Assays CHO cell membranes (15 μg) are preincubated at room temperature with various concentrations of competing ligand in 80 μL of HBSS supplemented with 10 mM HEPES, pH 7.3, 20 mL of [3H]PGD2 (160 Ci/mmol) is then added to a final concentration of 5 nM and incubated for an additional 60 min at room temperature. Reactions are terminated by the addition of 100 μL of ice-cold assay buffer to each well, followed by rapid filtration through Whatman GF/B glass fiber filters using a Unifilter Cell Harvester. The filters are washed six times with 300 μL/well of ice-cold buffer, and the plates are dried at room temperature for at least 60 min. The level of radioactivity retained on the filters is measured by using a Beta Trilux counter after the addition of scintillant.

Animal Study: [1]

Animal Models Sprague-Dawley rats
Formulation 10% DMSO/saline solution
Dosages 10 mg/kg
Administration Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Pettipher R, et al. J Pharmacol Exp Ther, 2012, 340(2), 473-482.

[2] Barnes N, et al. Clin Exp Allergy, 2012, 42(1), 38-48.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02560610 Not yet recruiting Severe Eosinophilic Asthma Atopix Therapeutics, Ltd. August 2016 Phase 2
NCT02341521 Completed Asthma Atopix Therapeutics, Ltd.|Simbec Research March 2015 Phase 1
NCT02002208 Active, not recruiting Atopic Dermatitis Atopix Therapeutics, Ltd. October 2013 Phase 2
NCT01056783 Completed Eosinophilic Esophagitis Oxagen Ltd August 2010 Phase 2
NCT01056575 Completed Healthy Volunteers Oxagen Ltd February 2010 Phase 1

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Chemical Information

Download OC000459 SDF Download OC000459 SDF
Molecular Weight (MW) 348.37
Formula

C21H17FN2O2

CAS No. 851723-84-7, 950688-14-9 (sodium salt)
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 4 mg/mL (11.48 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
* <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.
Chemical Name 1H-Indole-1-acetic acid, 5-fluoro-2-methyl-3-(2-quinolinylmethyl)-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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