PF-3716556

製品コードS2222 バッチS222202

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	C₂₂H₂₆N₄O₃
	分子量	394.47	CAS No.	928774-43-0
Solubility (25°C)*	体外	DMSO	78 mg/mL (197.73 mM)
		Ethanol	78 mg/mL (197.73 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 3716556 is a potent and selective P-CAB (potassium-competitive acid blocker), with pIC50 of 6.026 and 7.095 for the inhibition of porcine H⁺,K⁺-ATPase activity in ion-leaky and ion-tight assay, respectively, inhibits gastric acid secretion, displays no activity at Na⁺,K⁺-ATPase, used for the treatment of gastroesophageal reflux disease.
in vitro	PF-03716556 is a potent, and selective acid pump antagonist with pIC50 of about of 6.026 and 7.095 for the inhibition of porcine H⁺,K⁺-ATPase activity in ion-leaky and ion-tight assay, respectively. PF-03716556 is used for the treatment of gastroesophageal reflux disease. PF-03716556 is highly selective for H+, K+-ATPase in vitro, displays no activity at Na+, K+-ATPase. PF-03716556 has no species differences among the porcine, canine and human enzymes. PF-03716556 has a competitive and reversible mode of action.^[1]
in vivo	PF-03716556 inhibits gastric acid secretion in rat and dog models. PF-03716556 offers long-lasting and maximal efficacy within 30 min of a single dosing with responses that are maintained for at least 5 days of repeated dosing with no signs of tolerance. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	H⁺,K⁺-ATPase Activity
キナーゼアッセイ	H⁺,K⁺-ATPase activity in ion-leaky/ion-tight gastric vesicles (ion-leaky/ion-tight assay). Gastric H⁺,K⁺-ATPase activity is measured in a 60 μl reaction mixture containing either the test compound with 0.3 μg of freeze-dried vesicles, 5 mM KCl, 3 mM MgSO₄, 3 mM Na₂ATP, and 40 mM Bis-Tris, pH 6.4, at 37°C for ion-leaky assays or the test compound, 2 μg of vesicles, 150 mM KCl, 3 mM MgSO₄, 3 mM Na₂ATP, 17 μM valinomycin, and 5 mM Tris, pH 7.4, at 37°C for ion-tight assays, in 96-well clear polystyrene plates (nontissue culture-treated). For 0% inhibition and 100% inhibition controls, enzymatic reactions are performed in the presence of 1% DMSO and 100 μM SCH28080, respectively. Reaction mixtures are incubated at 37°C for 30 min in the presence of Na₂ATP; reactions are aborted by the addition of 30 μl of 10% SDS containing antifoam A. A colorimetric reagent is prepared by mixing 10% L-ascorbic acid, pH 5.0, and 35 mM ammonium molybdate in 15 mM zinc acetate, pH 5.0, at a ratio of 4:1. We then add 200 μl of colorimetric reagent to each well. After incubation at 37°C for 30 min (ion-leaky assays) or at 37°C for 20 min (ion-tight assays), the optical density of each well is measured at 750 nm using a plate reader. Inorganic phosphate solution containing KH₂PO₄ and K₂HPO₄ is used as a standard.
動物実験	動物モデル	rat
	投薬量	1–10 mg/kg; 1 ml/kg
	投与方法	i.v.

参考

[1] Mori H, et al. J Pharmacol Exp Ther, 2009, 328(2), 671-679.

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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