LY-2183240

製品コードS8052 バッチS805201

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

C17H17N5O
分子量 307.35 CAS No. 874902-19-9
Solubility (25°C)* 体外 DMSO 61 mg/mL (198.47 mM)
Ethanol 61 mg/mL (198.47 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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 LY-2183240 is a potent, covalent inhibitor of the EC-degrading enzyme fatty acid amide hydrolase (FAAH). LY-2183240 disrupts the cellular uptake of the lipid endocannabinoid (EC) anandamide and promote analgesia in vivo. LY-2183240 is also an inhibitor of monoacylgylcerol lipase (MGL).
in vitro

LY2183240 inhibits anandamide uptake in live cell with IC50 of 0.27 nM. [1] This compound inactivates FAAH by carbamylation of the enzyme’s serine nucleophile. It also inhibits KIAA1363, α/β-hydrolase 6 (Abh6) and monoacylglycerol lipase (MAG lipase) expressed in COS-7 cells with IC50 of 8.3, 0.09 and 5.3 nM, respectively. [2]
in vivo

LY2183240 (i.p.) results in a dose-dependent increase in anandamide concentrations in rat cerebellum with ED50 of 1.37 mg/kg. This compound (i.p.) dose-dependently attenuates formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms. [1] This chemical (10 mg/kg, i.p.) treatment for 90 min inactivates FAAH (100% inhibited), Abh6 (>90% inhibited), and MAG lipase (>60% inhibited) in brain tissue. [2] It shows beneficiation on fear-potentiated startle (FPS) and alcohol-seeking behaviors (HAP) in mice selectively bred for high alcohol preference. Repeated administration of this compound (30 mg/kg) reduces the expression of FPS in HAP mice when given prior to a second FPS test 48 h after fear conditioning. Both the 10 and 30 mg/kg doses of this chemical enhances the expression of alcohol-induced conditioned place preference and this effect persisted in the absence of the drug. [3]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 mouse brain membranes
濃度 0.001-10 μM
反応時間 10 min
実験の流れ

FAAH activity is measured in mouse brain membranes in the presence of varying concentrations of inhibitor. Brain membranes (1 mg/mL) from FAAH (-/-) mice are used as a control. Briefly, varying concentrations of this compound (1 μL, 100×stock in DMSO added to provide 0.001-10 μM final concentration) are preincubated with brain membranes (1 mg/mL in 50 mM Tris, pH 8, 94 μL) for 10 min.
動物実験 動物モデル male wild type or FAAH (-/-) C57Bl/6 mice
投薬量 10 mg/kg
投与方法 IP

参考

  • https://pubmed.ncbi.nlm.nih.gov/16314570/
  • https://pubmed.ncbi.nlm.nih.gov/16866524/
  • https://pubmed.ncbi.nlm.nih.gov/20838777/
  • https://pubmed.ncbi.nlm.nih.gov/18597752/

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。