GW6471

製品コードS2798 バッチS279806

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

C35H36F3N3O4
分子量 619.67 CAS No. 880635-03-0
Solubility (25°C)* 体外 DMSO 50 mg/mL (80.68 mM)
Ethanol 4 mg/mL (6.45 mM)
Water Insoluble
* <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 GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.
in vitro

GW6471 completely inhibits GW409544-induced activation of PPARα with IC50 of 0.24 μM. GW6471 at concentration ranging from 0.001-10 μM disrupts the interactions between PPAR and coactivator motifs derived from SRC-1 or CBP, but promotes the binding of the co-repressor motifs from SMRT or N-CoR. GW6471 adopts a U-shaped configuration and wraps around C276 of helix 3, destroys the integrity of the charge clamp but leaves sufficient space to accommodate the additional helical turn of the co-repressor motif in the PPAR/GW6471/SMRT complexes. [1]

GW6471 at concentration of 10 μM significantly prevents cardiomyocyte differentiation and results in the reduced expression of cardiac sarcomeric proteins (ie α-actinin, troponin-T) and specific genes (ie α-MHC, MLC2v) in a time-dependent manner through inhibiting PPARα. [2]
in vivo

GW6471 is a potent PPARα antagonist.

プロトコル(参考用のみ)

キナーゼアッセイ Binding assays
The effects of GW6471 on the interaction of coactivator and co-repressor peptides with PPAR are determined by chemical-mediated fluorescence energy transfer assays. The experiments are conducted with 5 nM PPARα LBD of biotinylated peptide containing individual motifs , following the manufacturer
細胞アッセイ 細胞株 Cell-free assays
濃度 0.24 μM
反応時間
実験の流れ
動物実験 動物モデル Male athymic Nu/Nu mice
投薬量 20 mg/kg
投与方法 i.p.

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：

Suppression of ferroptosis by vitamin A or radical-trapping antioxidants is essential for neuronal development [ Nat Commun, 2024, 15(1):7611] PubMed: 39218970
CD24 negativity reprograms mitochondrial metabolism to PPARα and NF-κB-driven fatty acid β-oxidation in triple-negative breast cancer [ Cancer Lett, 2024, 587:216724] PubMed: 38373689
Tubular CPT1A deletion minimally affects aging and chronic kidney injury [ JCI Insight, 2024, 9(6)e171961] PubMed: 38516886
PIM1 drives lipid droplet accumulation to promote proliferation and survival in prostate cancer [ Oncogene, 2024, 43(6):406-419] PubMed: 38097734
Oxidative stress in peroxisomes induced by androgen receptor inhibition through peroxisome proliferator-activated receptor promotes enzalutamide resistance in prostate cancer [ Free Radic Biol Med, 2024, 221:81-88] PubMed: 38762061
Astragaloside IV ameliorates cisplatin-induced liver injury by modulating ferroptosis-dependent pathways [ J Ethnopharmacol, 2024, 328:118080] PubMed: 38521426
Farnesoid X receptor activation by bile acids suppresses lipid peroxidation and ferroptosis [ Nat Commun, 2023, 14(1):6908] PubMed: 37903763
Farnesoid X receptor activation by bile acids suppresses lipid peroxidation and ferroptosis [ Nat Commun, 2023, 14(1):6908] PubMed: 37903763
Suppression of the gut microbiota-bile acid-FGF19 axis in patients with atrial fibrillation [ Cell Prolif, 2023, 56(11):e13488] PubMed: 37186335
Suppression of the gut microbiota-bile acid-FGF19 axis in patients with atrial fibrillation [ Cell Prolif, 2023, e13488.] PubMed: 37186335

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。