Home Endocrinology & Hormones GPR antagonist OC000459

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OC000459 GPR antagonist

Cat.No.S2822

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

Chemical Structure

Molecular Weight: 348.37

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Quality Control

Batch: S282201 DMSO]4 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.5%
99.5

Chemical Information, Storage & Stability

Molecular Weight 348.37 Formula

C21H17FN2O2

 Storage (From the date of receipt)
CAS No. 851723-84-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C2=C(N1CC(=O)O)C=CC(=C2)F)CC3=NC4=CC=CC=C4C=C3

Solubility

In vitro
Batch:

DMSO : 4 mg/mL ( (11.48 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
DP2 [1]
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. This compound also displaces [3H]PGD2 from membranes from human Th2 lymphocytes with Ki of 4 nM. It antagonizes PGD2-mediated calcium mobilization 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 antagonizes the effect of PGD2 competitively in both the isolated leukocyte preparation and heparinized 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. [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. This compound 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. It 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] This chemical (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, it improves the night-time symptom scores, reduces the geometric mean sputum eosinophil count and respiratory infections. [2] 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. [3]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02560610 Completed
Severe Eosinophilic Asthma
Chiesi Farmaceutici S.p.A.|Atopix Therapeutics Ltd.
 September 2016 Phase 2
NCT01056783 Completed
Eosinophilic Esophagitis
Oxagen Ltd
 August 2010 Phase 2
NCT01056575 Completed
Healthy Volunteers
Oxagen Ltd
 February 2010 Phase 1
NCT01448902 Completed
Allergic Rhinitis
Oxagen Ltd
 March 2007 Phase 2
NCT00290381 Completed
Allergic Rhinitis
Trevor Hansel|Oxagen Ltd|Imperial College London
 Phase 1|Phase 2

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