OC000459

製品コードS2822 バッチS282201

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₁H₁₇FN₂O₂
	分子量	348.37	CAS No.	851723-84-7
Solubility (25°C)*	体外	DMSO	4 mg/mL (11.48 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2.
in vitro	OC000459 inhibits the binding of [³H]PGD2 to membranes from CHO cells transfected with human DP2 with K_i of 13 nM. OC000459 also displaces [³H]PGD2 from membranes from human Th2 lymphocytes with K_i 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]

プロトコル(参考用のみ)

キナーゼアッセイ	Ligand Binding Assays
キナーゼアッセイ	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.
動物実験	動物モデル	Sprague-Dawley rats
	投薬量	10 mg/kg
	投与方法	Orally

参考

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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