URB597

製品コードS2631 バッチS263101

印刷

化学情報

Chemical Structure Synonyms KDS-4103 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H22N2O3
分子量 338.4 CAS No. 546141-08-6
Solubility (25°C)* 体外 DMSO 68 mg/mL (200.94 mM)
Ethanol 4 mg/mL (11.82 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.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.000mg/ml (2.96mM) Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 URB597（KDS-4103）は、他のカンナビノイド関連ターゲットには活性がない、IC50が4.6 nMの強力な経口生体利用可能なFAAH阻害剤です。フェーズ1。
in vitro URB597 binds in the hydrophobic pocket and catalytic core of FAAH that connects the active site residues to the membrane surface of FAAH. This compound inhibits FAAH activity in human liver microsomes with IC50 of 3 nM. It reduces the expression of the LPS-induced enzymes cyclo-oxygenase 2 (COX-2) and inducible nitric oxide synthase (iNOS; NOS2) in primary rat microglial cell, with a concomitant reduction in the release of the inflammatory mediators prostaglandin E2 (PGE2) and (NO) nitric oxide. This chemical evokes Ca2+ entry in HEK293-F Cells transiently expressing human or rat TRPA1 gene. It also activates Ca2+ entry in rat DRG neurons natively expressed TRPA1 channels.
in vivo URB597 inhibits [3H]anandamide hydrolysis in rat brain membranes with a parallel increase in brain anandamide, OEA, and PEA content by inhibition of FAAH. This compound enhances the hypothermia effect induced by ethanolamide by inhibiting FAAH. When delivered intraperitonealy (0.3 mg/kg) it reduces allodynia and hyperalgesia through cannabinoid CB1 and CB2 receptor-mediated analgesia in rats with inflammatory pain. This chemical reduces the reduction in body weight gain and sucrose intake induced by the chronic mild stress in rats through inhibition of brain FAAH activity. It could reverse most depressive-like symptoms induced by adolescent THC exposure in femal rats.

プロトコル(参考用のみ)

キナーゼアッセイ Pharmacology
Membrane fractions are prepared from brain homogenates, and FAAH activity is assayed using [3H]anandamide (anandamide[ethanolamine-3H], 60 Ci/mmol) as a substrate. Rat brain membranes (50 μg protein) are incubated for 30 min at 37 °C in buffer containing [3H]anandamide and varying concentrations of this compound. At the end of the incubation period, we stopp the reactions with a mixture of chloroform/methanol and measured [3H]ethanolamine in the aqueous phase by liquid scintillation counting.
動物実験 動物モデル Adult male Wistar rats (250–300 g) and C57/BL6 or FAAH-/- mice
投薬量 0.3 mg/kg
投与方法 Inject subcutaneously in a single dose 2 hours or 16 hours before killing

参考

  • https://pubmed.ncbi.nlm.nih.gov/15456244/
  • https://pubmed.ncbi.nlm.nih.gov/16834756/
  • https://pubmed.ncbi.nlm.nih.gov/17543306/
  • https://pubmed.ncbi.nlm.nih.gov/17314320/
  • https://pubmed.ncbi.nlm.nih.gov/15579492/
  • https://pubmed.ncbi.nlm.nih.gov/16331291/
  • https://pubmed.ncbi.nlm.nih.gov/17511970/
  • https://pubmed.ncbi.nlm.nih.gov/20850463/

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：

URB597 downregulates DJ-1 expression in the mouse striatum and induces neurodegeneration [ Exp Cell Res, 2025, 449(2):114602] PubMed: 40373851
FAAH Inhibition Counteracts Neuroinflammation via Autophagy Recovery in AD Models [ Int J Mol Sci, 2024, 25(22)12044] PubMed: 39596118
URB597 Administration decreases neuroinflammation and promotes autophagy in Alzheimer's disease models [ IRIS, 2023, ] PubMed: None
Endocannabinoids regulate cocaine-associated memory through brain AEA-CB1R signalling activation [ Mol Metab, 2022, 65:101597] PubMed: 36096452
Neuroprotective Effects of VEGF-A Nanofiber Membrane and FAAH Inhibitor URB597 Against Oxygen-Glucose Deprivation-Induced Ischemic Neuronal Injury [ Int J Nanomedicine, 2021, 16:3661-3678] PubMed: 34093011
Fatty Acid Amide Hydrolase (FAAH) Inhibition Modulates Amyloid-Beta-Induced Microglia Polarization [ Int J Mol Sci, 2021, 22(14)7711] PubMed: 34299330
Inhibition of fatty acid amide hydrolase prevents pathology in neurovisceral acid sphingomyelinase deficiency by rescuing defective endocannabinoid signaling [ EMBO Mol Med, 2020, e11776] PubMed: 33016621
p21-activated kinase 1 restricts tonic endocannabinoid signaling in the hippocampus [ Elife, 2016, 5e14653] PubMed: 27296803

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。