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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 | C19H16ClNO3 |
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分子量 | 341.79 | CAS No. | 1467057-23-3 | |
Solubility (25°C)* | 体外 | DMSO | 68 mg/mL (198.95 mM) | |
Ethanol | 68 mg/mL (198.95 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-06409577 is an orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms. |
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in vitro | PF-06409577 activates α1β1γ1 and α2β1γ1 AMPK isoforms with EC50 of 7.0 nM and 6.8 nM but was much less active against α1β2γ1/α2β2γ1/α2β2γ3 AMPK isoforms with EC50 greater 4000 nM[1]. |
in vivo | PF-06409577 exhibits efficacy in a preclinical model of diabetic nephropathy[1]. It exhibits high plasma protein binding in rat (plasma unbound fraction, fu,p = 0.0044), dog (fu,p = 0.028), monkey (fu,p = 0.032), and human (fu,p = 0.017). Following iv administration, PF-06409577 demonstrates moderate plasma clearance (CLp) in rats (22.6 mL/min/kg), dogs (12.9 mL/min/kg), and monkeys (8.57 mL/min/kg) and was well distributed with steady state distribution volumes (Vdss) ranging from 0.846-3.15 L/kg. Following oral administration of crystalline PF-06409577 in 0.5% methylcellulose suspension, PF-06409577 is rapidly absorbed (Tmax = 0.25-1.20 h) in rats, dogs, and monkeys. The corresponding oral bioavailability (F) values in rats, dogs, and monkeys, were 15%, 100%, and 59%, respectively. PF-06409577 is subject to a higher degree of first pass intestinal glucuronidation in the rat (relative to other preclinical species and human)[2]. |
動物実験 | 動物モデル | ZSF-1 rats |
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投薬量 | 100 mg/kg | |
投与方法 | by oral gavage |
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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。