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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | ||||||||
化学式 | C18H19N3O3 |
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分子量 | 325.36 | CAS No. | 2088410-46-0 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 65 mg/mL (199.77 mM) | ||||||||
Water | Insoluble | ||||||||||
Ethanol | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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 | GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics. |
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in vitro | GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 is capable of reducing the MCP-1 response in a concentration-dependent manner, providing strong evidence that GSK620 is indeed engaging BD2 in cells.[1] |
in vivo | GSK620 is a potent and selective pan-BD2 inhibitor with excellent in vivo PK properties and excellent developability properties, with the exception of moderate FaSSIF solubility driven by its highly crystalline nature.[1] |
細胞アッセイ | 細胞株 | human whole blood, hepatocytes |
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濃度 | 0.5 μM | |
反応時間 | 60 min, 120 min | |
実験の流れ | GSK620 is diluted in 100% DMSO to give a range of appropriate concentrations at 140× the required final assay concentration, of which 1 μL is added to a 96 well tissue culture plate. Then 130 μL of human whole blood, collected into sodium heparin anticoagulant (1 unit/mL final) is added to each well and plates are incubated at 37℃ (5% CO2) for 30 min before the addition of 10 μL of 2.8 μg/mL LPS, diluted in complete RPMI 1640 (final concentration 200 ng/mL), to give a total volume of 140 μL per well. After further incubation for 24 h at 37℃, 140 μL of PBS is added to each well. The plates are sealed, shaken for 10 min, and then centrifuged (2500 rpm × 10 min). Finally, 100 μL of the supernatant is removed and MCP-1 levels assayed immediately by immunoassay. |
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動物実験 | 動物モデル | Male Wistar Han rats, male Beagle dog |
投薬量 | 0.5 mg/kg, 1 mg/kg, 3 mg/kg | |
投与方法 | IV, 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。