Denifanstat (TVB-2640)

製品コードS9714 バッチS971402

印刷

化学情報

Chemical Structure Synonyms ASC-40, FASN-IN-2 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C27H29N5O
分子量 439.55 CAS No. 1399177-37-7
Solubility (25°C)* 体外 DMSO 88 mg/mL (200.2 mM)
Ethanol 88 mg/mL (200.2 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。

 4.400mg/ml (10.01mM) Taking the 1 mL working solution as an example, add 50 μL 88 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL 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 Denifanstat (TVB-2640) is an orally bioavailable, pharmacological fatty acid synthase (FAS/FASN) inhibitor with therapeutic potential in patients with NAFLD and nonalcoholic steatohepatitis.
in vitro

Denifanstat (TVB-2640) markedly inhibits SARS-CoV-2 with EC50s of 4 nM, and could strikingly inhibit SARS-CoV-2 new variants with similar inhibitory effects on the early-lineage SARS-CoV-2 (USA-WA1/2020) virus.[2]
in vivo

Denifanstat (TVB-2640) shows significant in vivo antiviral activity and protects SARS-CoV-2-infected mice for survival.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HEK293T-hACE2, Caco-2, MEF-hACE2 cells
濃度 100 nM for HEK293T-hACE2 cells; 2 µM for NCI-H1355, NCI-1437 and Caco-2 cells; 1 µM for MEF-hACE2 cells
反応時間 16+24 h
実験の流れ

Indicated cells were pre-treated with Denifanstat (TVB-2640) from 16 h before infection and then infected with SARS-CoV-2-mNG. Fluorescence images were acquired at 48 hpi. Hoechst 33342 was used for nuclear staining. Assessment of anti-SARS-CoV-2 ability of FAS inhibitors in multiple cell lines. Indicated cells were pre-treated with this compound and infected with SARS-CoV-2 for 24 h, after infection cells were collected for quantification of intracellular viral RNA by qPCR.

(Data sourced from selleck products)
動物実験 動物モデル K18-hACE2 transgenic mice infected by SARS-CoV-2
投薬量 8 mg kg-1 body weight
投与方法 i.p.

(Data sourced from selleck products)

参考

  • https://pubmed.ncbi.nlm.nih.gov/31630414/
  • https://pubmed.ncbi.nlm.nih.gov/34580494/

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：

Organismal metabolism regulates the expansion of oncogenic PIK3CA mutant clones in normal esophagus [ Nat Genet, 2024, 10.1038/s41588-024-01891-8] PubMed: 39169259
Formate promotes invasion and metastasis in reliance on lipid metabolism [ Cell Rep, 2023, 42(9):113034] PubMed: 37651228
FASN multi-omic characterization reveals metabolic heterogeneity in pancreatic and prostate adenocarcinoma [ J Transl Med, 2023, 21(1):32] PubMed: 36650542
Imaging the metabolic reprograming of fatty acid synthesis pathway enables new diagnostic and therapeutic opportunity for breast cancer [ Cancer Cell Int, 2023, 23(1):83] PubMed: 37120513
The Deubiquitinase USP13 Maintains Cancer Cell Stemness by Promoting FASN Stability in Small Cell Lung Cancer [ Front Oncol, 2022, 12:899987] PubMed: 35898882
Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication [ Nat Metab, 2021, 10.1038/s42255-021-00479-4] PubMed: 34580494
Metabolic convergence on lipogenesis in RAS, BCR-ABL, and MYC-driven lymphoid malignancies [ Cancer Metab, 2021, 9(1):31] PubMed: 34399819
Molecular response to PARP1 inhibition in ovarian cancer cells as determined by mass spectrometry based proteomics [ J Ovarian Res, 2021, 14(1):140] PubMed: 34686201
Molecular Response to PARP1 Inhibition in Ovarian Cancer Cells as Determined by Mass Spectrometry Based Proteomics [ bioRxiv, 2021, 10.1101/2021.03.12.435005] PubMed: None

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。