Name: OC000459
Brand: Selleck Chemicals
SKU: S2822
Rating: 5 (1 reviews)

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.5

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR
Other GPR Inhibitors	ONC212 Fasiglifam(TAK-875) Hemihydrate GW9508 AH7614 3-chloro-5-hydroxybenzoic Acid JMS-17-2 GSK1292263 AZD1981 TC-G-1008 (GPR39-C3) SNAP94847 hydrochloride

Chemical Information, Storage & Stability

Molecular Weight	348.37	Formula	C₂₁H₁₇FN₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	851723-84-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	DP2 13 nM
In vitro	OC000459 inhibits the binding of [³H]PGD2 to membranes from CHO cells transfected with human DP2 with K_i of 13 nM. This compound also displaces [³H]PGD2 from membranes from human Th2 lymphocytes with K_i 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22106101/ [2] https://pubmed.ncbi.nlm.nih.gov/21762224/ [3] https://pubmed.ncbi.nlm.nih.gov/22496329/

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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OC000459 GPR antagonist

Chemical Structure

Molecular Weight: 348.37