GSK620

製品コードS9685 バッチS968502

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C18H19N3O3
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
* <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 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.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 human whole blood, hepatocytes
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.
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

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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