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| | [4-クロロ-6-(2,3-キシリジノ)-2-ピリミジニルチオ]酢酸 製品概要 |
| 化学名: | [4-クロロ-6-(2,3-キシリジノ)-2-ピリミジニルチオ]酢酸 | | 英語化学名: | WY-14643 | | 别名: | WY-14643/WY14643;((4-chloro-6-((2,3-dimethylphenyl)amino)-2-pyrimidinyl)thio)-aceticaci;((4-chloro-6-(2,3-xylidino)-2-pyrimidinyl)thio)-aceticaci;4-chloro-6-(2,3-xylidino)-2-*pyrimidinylthioaceti;pirnixicacid;NSC 310038;Acetic acid, 2-[[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]-;wyeth14,643 | | CAS番号: | 50892-23-4 | | 分子式: | C14H14ClN3O2S | | 分子量: | 323.8 | | EINECS: | | | カテゴリ情報: | Inhibitors;Intracellular receptor;Inhibitor | | Mol File: | 50892-23-4.mol | ![[4-クロロ-6-(2,3-キシリジノ)-2-ピリミジニルチオ]酢酸](CAS/GIF/50892-23-4.gif) |
| | [4-クロロ-6-(2,3-キシリジノ)-2-ピリミジニルチオ]酢酸 物理性質 |
| 融点 | 155°C | | 沸点 | 514.4±50.0 °C(Predicted) | | 比重(密度) | 1.2984 (rough estimate) | | 屈折率 | 1.5630 (estimate) | | 貯蔵温度 | Keep in dark place,Sealed in dry,Room Temperature | | 溶解性 | Soluble in DMSO (up to 40 mg/ml). | | 外見 | White crystalline solid | | 酸解離定数(Pka) | 2.99±0.10(Predicted) | | 色 | Off-white | | 安定性： | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 6 months. |
| | [4-クロロ-6-(2,3-キシリジノ)-2-ピリミジニルチオ]酢酸 Usage And Synthesis |
| 外観 | 白色～うすい黄色粉末～結晶 | | 説明 | WY-14643 (50892-23-4) is a selective PPARα agonist (EC50=0.63, 32 and >100 μM for PPARα,γ and δ, respectively).1? Displays anti-inflammatory activity2 and reduces LPS-induced inflammation in alveolar epithelial cells3. Induces “browning” of white adipocytes in combined treatment with retinoic acid.4? Stimulates ADAM10-mediated proteolysis of? amyloid precursor protein in a mouse model.5 Down regulates NFkB transcriptional activity. Review.6 | | 使用 | A highly potent PPARα agonist | | 使用 | WY-14643 has been used:
- as a positive control for transfection and luciferase assay
- to stimulate bone marrow–derived macrophages (BMDM) for autophagic flux analysis
- to analyze the regulation of fatty acid metabolism-immune nexus (FAMIN) expression in cell culture
| | 定義 | ChEBI: Pirinixic acid is a member of pyrimidines, an organochlorine compound and an aryl sulfide. It is functionally related to an acetic acid. | | 一般的な説明 | WY-14643 prevents lipopolysaccharide (LPS)-induced inflammation in synovial fibroblasts. It protects cortical neurons from pro-inflammatory mediator-induced cell injuries. WY-14643 has inhibitory effects on pro-inflammatory responses in microglia. It improves oxido-nitrosative stress in disease models and reduces the generation of reactive oxygen species (ROS), nitric oxide (NO) and lipid peroxidation end-products in the brain. | | 生物活性 | Selective PPAR α agonist (EC 50 values are 0.63, 32 and > 100 μ M at PPAR α , PPAR γ and PPAR δ respectively). Negatively inhibits NF- κ B transcriptional activity and decreases the inflammatory response in vitro and in vivo . | | Biochem/physiol Actions | Selective PPARα agonist. | | 安全性プロファイル | Moderately toxic by
ingestion. Suspected carcinogen with
experimental carcinogenic and tumorigenic
data. Mutation data reported. When heated
to decomposition it emits very toxic fumes
of Cl-, NOx and SOx | | 貯蔵 | Store at RT | | 参考文献 | 1) Forman et al. (1997), Hypolipidemic drugs, polyunsaturated fatty acids and eicosanoids are ligands for peroxisome proliferator-activated receptors alpha and delta; Proc. Natl. Acad. Sci. USA, 94 4312
2) Devchand et al. (1996), The PPARalpha-leukotriene B4 pathway to inflammation control; Nature, 384 39
3) Heckler et al. (2015), PPAR-a activation reduced LPS-induced inflammation in alveolar epithelial cells; Exp. Lung Res., 41 393
4) Wang et al. (2015), WY14643 combined with all-trans retinoic acid acts via p38 MAPK to induce “browning” of white adipocytes in mice; Genet. Mol. Res., 14 6978
5) Corbett et al. (2015), Activation of peroxisome proliferator-activated receptor alpha stimulates ADAM10-mediated proteolysis of APP; Proc. Natl. Acad. Sci. USA, 112 8445
6) Merk et al. (2015), Pirinixic acids: flexible fatty acid mimetics with various biological activities; Future Med. Chem., 7 1597 |
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