GW501516

製品コードS1473 バッチS147302

印刷

化学情報

Chemical Structure Synonyms GW 1516 ,GSK-516 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H18F3NO3S2
分子量 453.50 CAS No. 317318-70-0
Solubility (25°C)* 体外 DMSO 91 mg/mL (200.66 mM)
Ethanol 22 mg/mL (48.51 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。

 4.550mg/ml (10.03mM) Taking the 1 mL working solution as an example, add 50 μL of 91 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. 
Clear solution
5% DMSO 95% Corn oil

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。

 1.500mg/ml (3.31mM) Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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 GW501516 is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. Phase 4.
in vitro GW501516 is demonstrated to be 1000-fold more selective in comparison to existing subtypes. This compound increases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux In macrophages, fibroblasts, and intestinal cells. [2] It can regulate expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. [4] Additionally, this chemical is shown to block insulin resistance and fatty acid-induced nuclear factor-κB activation. [5] It reduces the IFNγ-induced up-regulation of TNFα and inducible NO synthase, and showed anti-inflammatory activity. [6]
in vivo GW501516 dramatically increases serum high density lipoprotein cholesterol while lowering the levels of small-dense low density lipoprotein, fasting triglycerides, and fasting insulin when dosed to insulin-resistant middle-aged obese rhesus monkeys. [2] This compound induces fatty acid β-oxidation in L6 myotubes and in mouse skeletal muscles. Its treatment to mice fed a high-fat diet ameliorates diet-induced obesity as well as insulin resistance. This chemical also dramatically improves diabetes, as demonstrated by the decrease in plasma glucose and blood insulin levels in genetically obese ob/ob mice. [7]
特徴 A selective PPARδ agonist compared with a synthetic LXRα agonist GW3965.

プロトコル(参考用のみ)

キナーゼアッセイ FA Binding Assays
The PPARα, γ, and δ ligand-binding domains are expressed in E. coli as polyhistidine-tagged fusion proteins. The proteins are purified, biotinylated, and immobilized on streptavidin-modified SPA beads. [3H]this compound is used as radioligands for determination of binding to PPARα, γ, and δ, respectively. The buffer for all assays is 50 mM HEPES (pH 7), 50 mM KCl, 5 mM CHAPS, 0.1 mg/mg BSA, and 10 mM DTT.
動物実験 動物モデル Male obese rhesus monkey
投薬量 0.1, 0.3, 1.0, and 3.0 mg/kg
投与方法 Orally

参考

  • https://pubmed.ncbi.nlm.nih.gov/12699745/
  • https://pubmed.ncbi.nlm.nih.gov/11309497/
  • https://pubmed.ncbi.nlm.nih.gov/10198642/
  • https://pubmed.ncbi.nlm.nih.gov/14525954/
  • https://pubmed.ncbi.nlm.nih.gov/20185762/
  • http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2687435/
  • https://pubmed.ncbi.nlm.nih.gov/14676330/

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：

Anlotinib Combined with Anti‐PD1 Potentiates Anti‐Tumor Immunity via Immunogenic Cell Death and Macrophage Reprogramming [ Adv Ther-Germany, 2023, 6, 2300141 ] 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。