受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H26N4O3 |
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分子量 | 394.47 | CAS No. | 928774-43-0 | |
Solubility (25°C)* | 体外 | DMSO | 79 mg/mL (200.26 mM) | |
Ethanol | 79 mg/mL (200.26 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. |
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. |
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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] |
キナーゼアッセイ | H+,K+-ATPase Activity | |
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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. |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。