WY-14643 (Pirinixic Acid)

製品コードS8029 バッチS802902

印刷

化学情報

Chemical Structure Synonyms NSC 310038 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C14H14ClN3O2S
分子量 323.8 CAS No. 50892-23-4
Solubility (25°C)* 体外 DMSO 64 mg/mL (197.65 mM)
Ethanol 64 mg/mL (197.65 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 WY-14643 (Pirinixic Acid, NSC 310038) is a potent and selective PPARα activator with an EC50 of 1.5 μM.
in vitro

WY 14643 (10 μM) almost completely inhibits interleukin-1-induced production of interleukin-6 and prostaglandin and expression of cyclooxygenase-2 in aortic smooth-muscle cells, through repression of NF-κB signaling. [2] WY14643 (250 μM) reduces VCAM-1 expression levels significantly, to 52 % of TNF-α-stimulated human endothelial cells. Pretreatment of endothelial cells with WY 14643 (10 μM) before TNF-α stimulation reduces U937 cell adhesion by 50%. [3]
in vivo

WY 14643 (1 mg/kg i.v. bolus) administration at 30 min before left anterior descending occlusion, causes significant reduction in infarct size of ∼44% in rats subjected to regional myocardial ischemia (25 min) and reperfusion (2 h). [4] WY 14643 (3 mg/kg) lowers basal plasma levels of glucose, triglycerides (-16% vs. untreated), and leptin (-52%), and also muscle triglyceride (-34%) and total long-chain acyl-CoAs (LCACoAs) (-41%) in high fat-fed rats. WY14643 substantially reduces visceral fat weight and total liver triglyceride content without increasing body weight gain. WY14643 enhances whole body insulin sensitivity (clamp glucose infusion rate increases 35% and glucose disposals 22%, vs. untreated). WY 14643 enhances insulin-mediated muscle glucose metabolic index (Rg') in red (47%) and white (63%) muscles as well as in white adipose tissue (90%), and reduces muscle triglyceride and LCACoA accumulation. [5]

プロトコル(参考用のみ)

キナーゼアッセイ PPAR activation assay
COS1 cells (3 × 105) are seeded into 9-cm-diameter plates in phenol red-free medium supplemented with 5% fetal calf serum stripped of endogenous steroid by treatment with dextran-coated charcoal. After 3 days the medium is replaced and CsCl purified plasmid DNA (10 μg) added by calcium phosphate precipitation. Each plate contains a CAT reporter gene (1 μg), an expression vector (PPAR, 1 μg), the β-galactosidase expression vector, PCH110 and pBluescribe M13 + DNA as a carrier (5 μg). Ligand (1000 × stocks in DMSO) is added 30 min after transfection. After a further 20 hr the cells are washed and fresh ligand added. After an additional 24 hr, cell extracts are prepared by three cycles of freeze-thawing and assayed forβ-galactosidase activity which is used to normalize the CAT assays. Extracts corresponding to 2 units of β-galactosidase activity are used for the CAT assay with 0.1 μCi of [14C]chloramphenicol (50 mCi/mmol) for 1 hr at 37 ℃. The acetylated chloramphenicol is separated by chromatography on silica gelTLC plates. The acetylated chloramphenicol is excised and counted in 5 mL of scintillation fluid.

カスタマーフィードバック

Data from [Data independently produced by , , Diabetes, 2017, 66(8):2112-2123]

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：

mTORC2 Facilitates Liver Regeneration Through Sphingolipid-Induced PPAR-α-Fatty Acid Oxidation [ Cell Mol Gastroenterol Hepatol, 2022, 14(6):1311-1331] PubMed: 35931382
Oroxylin A ameliorates AKI-to-CKD transition through maintaining PPARα-BNIP3 signaling-mediated mitochondrial homeostasis [ Front Pharmacol, 2022, 13:935937] PubMed: 36081929
Overexpression CPT1A reduces lipid accumulation via PPARα/CD36 axis to suppress the cell proliferation in ccRCC [ Acta Biochim Biophys Sin (Shanghai), 2022, 54(2):220-231] PubMed: 35130611
Critical role of peroxisome proliferator-activated receptor α in promoting platelet hyperreactivity and thrombosis under hyperlipidemia [ Haematologica, 2021, 10.3324/haematol.2021.279770] PubMed: 34615341
PPARα agonist WY-14,643 enhances ethanol metabolism in mice: Role of catalase [ Free Radic Biol Med, 2021, 169:283-293] PubMed: 33892114
CircRNA hsa_circ_0110102 inhibited macrophage activation and hepatocellular carcinoma progression via miR-580-5p/PPARα/CCL2 pathway [ Aging (Albany NY), 2021, 13(8):11969-11987] PubMed: 33891564
Fatter or stronger: Resource allocation strategy and the underlying metabolic mechanisms in amphibian tadpoles [ Comp Biochem Physiol Part D Genomics Proteomics, 2021, 38:100825] PubMed: 33770735
MDM2 and MDMX promote ferroptosis by PPARα-mediated lipid remodeling. [ Genes Dev, 2020, 34(7-8):526-543] PubMed: 32079652
Critical Biomarkers for Myocardial Damage by Fine Particulate Matter: Focused on PPARα-regulated Energy Metabolism [ Environ Pollut, 2020, 29;264:114659] PubMed: 32380395
Dehydroabietic Acid Alleviates High Fat Diet-Induced Insulin Resistance and Hepatic Steatosis Through Dual Activation of PPAR-γ and PPAR-α [ Biomed Pharmacother, 2020, 127:110155] PubMed: 32413669

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。