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WY-14643 (Pirinixic Acid)是一种有效的过氧化物酶体增殖子和PPARα激活剂，EC50为1.5 μM。
别名：Pirinixic Acid
WY-14643 (Pirinixic Acid)是一种有效的过氧化物酶体增殖子和PPARα激活剂，EC50为1.5 μM。WY 14643 (10 μM)作用于主动脉平滑肌细胞，通过抑制NF-κB信号通路，几乎完全抑制IL-1诱导的IL-6和前列腺素的产生，及环氧合酶-2的表达。WY14643 (250 μM)作用于TNF-α刺激的人类内皮细胞，显著降低VCAM-1表达水平，降低52%。使用WY 14643 (10 μM)预处理内皮细胞，再使用TNF-α刺激，降低50%U937细胞粘附。
| 细胞实验 | |
|---|---|
| 细胞系 | U937 cells |
| 方法 | Adhesion Assay. ECs were grown to confluence in 96-well plates, pretreated with PPARα activators for 24 hours, and stimulated with TNF-α for 8 hours, then adhesion assays were performed.19 Briefly, U937 cells were labeled with 2',7'-bis(2-carboxy)-fluorescein acetoxymethyl ester (Molecular Probes) and then added, under rolling conditions (63 rpm, 23°C, 15 minutes), to a rinsed EC monolayer (2×106 cells/mL) in RPMI medium/10% FCS/1 mmol/L CaCl2. Nonadherent cells were removed by inverting the plate under rotation (20 minutes). After solubilization of well contents, fluorescence intensity was measured in a microtiter plate fluorimeter (Pandex, FCA). A standard curve using dilutions of labeled U937 cells was determined, and results were expressed as cells/cm2. |
| 浓度 | 250 µmol/L |
| 处理时间 | 24 h |
| 动物实验 | |
|---|---|
| 动物模型 | Homozygous obese (Ob) Zucker rats model of partial (~70%) hepatic warm ischemia |
| 配制 | saline |
| 剂量 | 10 mg/kg |
| 给药处理 | intravenously |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
| 分子量 | 323.8 |
| 分子式 | C14H14ClN3O2S |
| CAS号 | 50892-23-4 |
| 纯度 | 99.22% |
| 溶解性（25°C） | DMSO 55 mg/mL |
| 储存和运输条件 |
固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.0883 mL | 15.4416 mL | 30.8833 mL |
| 5 mM | 0.6177 mL | 3.0883 mL | 6.1767 mL |
| 10 mM | 0.3088 mL | 1.5442 mL | 3.0883 mL |
Cell Rep. 2019 Dec 17;29(12):4127-4143.e8.
SIRT6 Promotes Hepatic Beta-Oxidation via Activation of PPARα.
WY 14643购买自AbMole
 |
数据来源 | J Mol Neurosci (2016). Figure 6. WY 14643 |
| 方法 | western blot | |
| 细胞系 | Ik-B | |
| 浓度 | 10, 100 μM | |
| 处理时间 | 24 h | |
| 实验结果 | Decreasing of phosphorylated IkB and increasing of total IkB protein level were also observed following WY- 14643 treatment (Fig. 6), indicating that the phosphorylation, ubiquitination, and degradation of IkB induced by LPS was inhibited by WY-14643. |
 |
数据来源 | J Mol Neurosci (2016). Figure 1. WY 14643 |
| 方法 | real-time PCR | |
| 细胞系 | Ik-B | |
| 浓度 | 10, 100 μM | |
| 处理时间 | 24 h | |
| 实验结果 | In PPAR-α-specific siRNA-transfected cells, WY-14643 was unable to induce the expression of PPAR-α |
PPARα Agonist WY-14643 Induces SIRT1 Activity in Rat Fatty Liver Ischemia-Reperfusion Injury.
Pantazi E, et al. Biomed Res Int. 2015;2015:894679. PMID: 26539534.
PPARalpha activators inhibit cytokine-induced vascular cell adhesion molecule-1 expression in human endothelial cells.
Marx N, et al. Circulation. 1999 Jun 22;99(24):3125-31. PMID: 10377075.
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