PF-04620110

製品コードS7192 バッチS719201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H24N4O4
分子量 396.44 CAS No. 1109276-89-2
Solubility (25°C)* 体外 DMSO 49 mg/mL warmed with 50ºC water bath (123.6 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 PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
in vivo In Rats, PF-04620110 reduces plasma triglyceride levels t doses of ≥0.1 mg/kg following a lipid challenge. [1] DGAT1 inhibition by PF-04620110 causes an enrichment of polyunsaturated fatty acids within the TG class of lipids in rodents. [2]

プロトコル(参考用のみ)

キナーゼアッセイ In Vitro Assay for DGAT-1 Enzyme Inhibition
Human full-length diacylglycerol:acylCoA acyltransferase 1 (DGAT-1) is expressed in Sf9 insect cells which are then lysed and a crude membrane fraction is prepared. DGAT-1 activity was measured in 384-well format in a total assay volume of 25 μL that contained, Hepes buffer (50 mM, pH7.5), MgCl2 (10 mM), bovine serum albumin (0.6 mg/ml), [14C]decanoylCoA (20 μM, 58 Ci/mol) and membranes (25 μg/ml) into which 1,2 dioleoyl-sn-glycerol (75 μM) in acetone has already been incorporated. The inhibitors are present at a range of eight concentrations to generate an apparent IC50 for each compound. The reactions are allowed to proceed for 1.5 h at room temperature and then terminated by the addition of 10 μl of HCl (0.5 M). Reaction mixtures are neutralized by the addition of 15μl of tris(hydroxy-methyl)aminomethane (1M, pH 8.0) and then mixed by trituration with 37.5 μl of Microscint™-E. Plates contents are allowed to partition for 15 to 30 min before 14C was measured in a scintillation spectrometer.
動物実験 動物モデル Male Sprague Dawley rats
投薬量 ~10 mg/kg
投与方法 p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Pharmacokinetics and metabolism of GW9508 in rat by liquid chromatography/electrospray ionization tandem mass spectrometry. [ J Pharm Biomed Anal, 2019, 170:176-186] PubMed: 30927663
Rab18 promotes lipid droplet (LD) growth by tethering the ER to LDs through SNARE and NRZ interactions. [ J Cell Biol, 2018, 217(3):975-995] PubMed: 29367353

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。