GW9662

製品コードS2915 バッチS291502

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

C13H9ClN2O3
分子量 276.68 CAS No. 22978-25-2
Solubility (25°C)* 体外 DMSO 55 mg/mL (198.78 mM)
Water Insoluble
Ethanol 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 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。

 9.000mg/ml (32.53mM) Taking the 1 mL working solution as an example, add 50 μL of 180 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. 
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。

 0.150mg/ml (0.54mM) Taking the 1 mL working solution as an example, add 50 μL of 3 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 GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.
in vitro

GW9662 binds to Cys(285) on PPARgamma which is conserved among all three PPARs. This compound acts as an antagonist of PPARgamma which is confirmed in an assay of adipocyte differentiation inhibition. [1] It prevents activation of PPARγ and inhibits growth of human mammary tumour cell lines (MCF7, MDA-MB-468, MDA-MB-231) with IC50 of 20 μM-30 μM, suggesting either the existence of PPARγ agonistic properties of this chemical or growth-inhibitory mechanisms independent of PPARγ. Co-treatment with this compound (10 μM) results in statistically lower viable cell numbers after 7 days in MDA-MB-231 cells. [2] PPARγ1 ligands could suppress RANKL-induced osteoclast formation in primary murine myeloid (BMs) and RAW264.7 cells. Importantly, suppression by these ligands is reversed in a concentration-dependent fashion with this chemical (2 μM). It (2 μM) blocks IL-4 suppression of osteoclast formation in BMs. This compound (1 μM) blocks RANKL activation of NF-κB in RAW264.7 cells. [3] GW9662 (10 μM) inhibits hormone- and agonist-induced adipogenesis of primary preadipocytes from patients with thyroid eye disease. [4]
in vivo

Pretreatment with LPS (1 mg/kg i.p.) significantly attenuates all markers of renal injury and dysfunction caused by ischemia/reperfusion (I/R) injury in rats. Most notably, this compound (1 mg/kg i.p.) abolishes the protective effects of LPS. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
The human PPARα, PPARγ, and PPARδ ligand binding domains (LBDs) are expressed in E. coli as polyhistidine-tagged fusion proteins. Receptors are immobilized on SPA beads by addition of the desired receptor (15 nM) to a slurry of streptavidin-modifed SPA beads (0.5 mg/mL) in assay buffer. The mixture is allowed to equilibrate for at least 1 hour at room temperature, and the beads are pelleted by centrifugation at 1×103 g. The supernate is discarded, and the beads are resuspended in the original volume of fresh assay buffer with gentle mixing. The centrifugation/resuspension procedure is repeated, and the resulting slurry of receptor-coated beads is used immediately or stored at 4 ℃ for up to 1 week before use. [3H]GW2443 are used as radioligands for determination of competition binding to PPARα, PPARγ, and PPARδ, respectively. Unless otherwise indicated, the buffer used for all assays is 50 mM HEPES (pH 7), 50 mM NaCl, 5 mM CHAPS, 0.1 mg/mL BSA, and 10 mM DTT. For some experiments, the HEPES (pH 7) is replaced with 50 mM Tris (pH 8).
細胞アッセイ 細胞株 MDA-MB-231 cells
濃度 10 μM
反応時間 10 days
実験の流れ

MDA-MB-231 cells are seeded at a density of 1 × 105 cells per 25 cm3 tissue culture flask. After 24 h (day 0), the growth medium is replaced with fresh medium containing GW9662 (10 μM) or both together. Control flasks receives 0.1% DMSO. Cells are harvested on days 0, 3, 5, 7, 10 for each treatment condition by trypsinisation, stained using trypan blue, and the total and viable number of cells per flask calculates using a haemocytometer.
動物実験 動物モデル male Wistar rats
投薬量 1 mg/kg
投与方法 intraperitoneal injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/12022867/
  • https://pubmed.ncbi.nlm.nih.gov/15533890/
  • https://pubmed.ncbi.nlm.nih.gov/11226258/
  • https://pubmed.ncbi.nlm.nih.gov/12519830/
  • https://pubmed.ncbi.nlm.nih.gov/16014029/

カスタマーフィードバック

Data from [Data independently produced by , , Theranostics, 2018, 8(15):4262-4278]

Data from [Data independently produced by , , Sci Rep, 2016, 6:36382.]

Data from [Data independently produced by , , Toxicol Appl Pharmacol, 2016, 316:17-26.]

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：

Extracellular Vesicles From Limosilactobacillus johnsonii Enhance Milk Fat Synthesis by Inducing CD36 Dynamic Palmitoylation and Activating PPARγ Signalling [ J Extracell Vesicles, 2025, 14(8):e70143] PubMed: 40767021
LPS pretreated dental follicle stem cell derived exosomes promote periodontal tissue regeneration via miR-184 and PPARα-Akt-JNK signaling pathway [ Stem Cell Res Ther, 2025, 16(1):347] PubMed: 40605003
IRF8 aggravates nonalcoholic fatty liver disease via BMAL1/PPARγ axis [ Genes Dis, 2025, 12(3):101333] PubMed: 40083324
Epigenetic reprogramming via EZH2 inhibition rescues fibroadipose pathogenesis in secondary lymphedema through activating PPARγ signaling [ J Orthop Translat, 2025, 55:309-322] PubMed: 41079990
Compromised Peroxisome Proliferator-Activated Receptor γ-Mediated Impaired Placental Glucose Transport Via the Phosphatidylinositol 3-Kinase/Protein Kinase B Signaling Pathway Is Associated With Fetal Growth Restriction [ Lab Invest, 2025, 105(4):104103] PubMed: 39909142
TFPI2 hypermethylation promotes diabetic atherosclerosis progression through the Ap2α/PPARγ axis [ J Mol Cell Cardiol, 2025, 198:45-59] PubMed: 39631358
Naringin mitigates experimental autoimmune prostatitis by modulating oxidative stress and the NLRP3 inflammasome via the PPAR-γ/NF-κB pathway [ Sci Rep, 2025, 15(1):20843] PubMed: 40594232
FFAR2 expressing myeloid-derived suppressor cells drive cancer immunoevasion [ J Hematol Oncol, 2024, 17(1):9] PubMed: 38402237
Brain Short-Chain Fatty Acids Induce ACSS2 to Ameliorate Depressive-Like Behavior via PPARγ-TPH2 Axis [ Research (Wash D C), 2024, 7:0400] PubMed: 38939042
IL-33 Accelerates Chronic Atrophic Gastritis through AMPK-ULK1 Axis Mediated Autolysosomal Degradation of GKN1 [ Int J Biol Sci, 2024, 20(6):2323-2338] PubMed: 38617533

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。

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