PF-4136309

製品コードS8361 バッチS836101

化学情報

	Synonyms	INCB8761, PF-04136309	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₉H₃₁F₃N₆O₃
	分子量	568.59	CAS No.	857679-55-1
Solubility (25°C)*	体外	DMSO	100 mg/mL (175.87 mM)
		Ethanol	100 mg/mL (175.87 mM)
		Water	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	PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2.
in vitro	PF-4136309 is potent in inhibiting CCR2 mediated signaling events such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation. <sup><a class="sref" href="#s_ref">[1]</a></sup>
in vivo	PF-4136309 exhibits >100-fold selectivity over other homologous chemokine receptors, a free fraction of 24% in human serum and 15% in mouse serum, and an oral bioavailability of 47% in mice, suitable as a tool compound for target validation in rodent models.<sup><a class="sref" href="#s_ref">[2]</a></sup>

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Human PBMCs
	濃度	0.001 μM –10 μM
	反応時間	30 min
	実験の流れ	500,000 HPBMCs in serum free DMEM media are incubated with or without PF-4136309 and warmed to 37 °C. 400 μL of warmed 10 nM MCP-1 is added to the bottom chamber in all wells except the negative control. An 8 micron membrane filter is placed on top and the chamber lid is closed. Cells are then added to the holes in the chamber lid which are associated with the chamber wells below the filter membrane. The whole chamber is incubated at 37 °C, 5% CO2 for 30 min. The cells are then aspirated off, the chamber lid opened, and the filter gently removed. The filter is air dried and stained with Wright Geimsa stain. Filters are counted by microscopy. Antagonist potency is determined by comparing the number of cells that migrate to the bottom chamber in wells which contained antagonist, to the number of cells which migrate to the bottom chamber in MCP-1 control wells.
動物実験	動物モデル	Rats, Dogs
	投薬量	2 mg/kg
	投与方法	I.v.

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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