WY-14643 (Pirinixic Acid)
(Synonyms: 匹立尼酸,WY 14643,WY14643) 目录号 : GC14403
PPAR activator
Cas No.:50892-23-4
Sample solution is provided at 25 µL, 10mM.
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WY-14643, also known as Pirinixic Acid, has an agonistic action as peroxisome proliferator-activated receptor (PPAR). It is shown that aliphatic α-substitution of WY-14643 enhances both PPARα and PPARγ agonism. It has been demonstrated that aliphatic substitution in a-position to the carboxylic acid head group of WY-14643 improves both PPARa and PPARg activity and leads to balanced dual PPARa/g agonists in the lower micromolar range, with a-hexyl pirinixic acid as the most active compound. WY-14,643 can moderately elevate the level of TNFa mRNA in the liver. WY-14,643 stimulates production of low levels of hepatic TNFα by Kupffer cells which acts indirectly as a hepatocyte mitogen.
Reference
[1].Laura Popescu, Oliver Rau, Jark Böttcher, Yvonne Syha, Manfred Schubert-Zsilavecz. Quinoline-Based Derivatives of Pirinixic Acid as Dual PPAR α/γ Agonists. Archiv der Pharmazie. Volume 340, Issue 7, pages 367–371, July 2007
[2].Heiko Zettl, Michaela Dittrich, Ramona Steri, Ewgenij Proschak, Oliver Rau, Dieter Steinhilber, Gisbert Schneider, Michael Lämmerhofer, Manfred Schubert-Zsilavecz. Novel Pirinixic Acids as PPARα Preferential Dual PPARα/γ Agonists. QSAR & Combinatorial Science. Volume 28, Issue 5, pages 576–586, May 2009
[3].Heidi K.Bojes, Dori R.Germolec, Petia Simeonova, Alessandria Bruccoleri, Robert Schoonhoven, Michael I.Luster, Ronald G.Thurman. Antibodies to tumor necrosis factor alpha prevent increases in cell replication in liver due to the potent peroxisome proliferator, WY-14,643. Carcinogenesis (1997) 18 (4): 669-674.
| Cell experiment [1]: | |
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Cell lines |
Human ECs and U937 cells |
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Preparation method |
The solubility of this compound in DMSO is > 16.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0, 2.5, 25 or 250 μM; 24 hrs |
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Applications |
Pretreatment of ECs with 250 μM WY-14643 significantly down-regulated the VCAM-1 expression level to 52 ± 2% of TNF-α-stimulated cells. Besides, pretreatment of ECs with WY-14643 before TNF-α stimulation significantly reduced U937 cell adhesion to 37.3 ± 4.3 × 103 cells/cm2. Northern blot analysis indicated that the increased VCAM-1 mRNA level caused by TNF-α stimulation could be concentration-dependently inhibited by pretreatment with WY-14643. |
| Animal experiment [2]: | |
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Animal models |
High fat-fed rats |
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Dosage form |
3 mg/kg/day; p.o.; for 2 weeks |
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Applications |
In high fat-fed rats, WY-14643 lowered basal plasma levels of glucose, triglycerides and leptin, muscle triglyceride as well as total LCACoAs. Besides, WY-14643 significantly reduced visceral fat weight and total liver triglyceride content, without increasing body weight gain. In addition, WY-14643 enhanced whole body insulin sensitivity, thus increasing insulin-mediated muscle glucose metabolic index in red and white muscles as well as in white adipose tissue, and reducing muscle triglyceride as well as LCACoA accumulation. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Marx N, Sukhova GK, Collins T, Libby P, Plutzky J. PPARalpha activators inhibit cytokine-induced vascular cell adhesion molecule-1 expression in human endothelial cells. Circulation. 1999 Jun 22;99(24):3125-31. [2]. Ye JM, Doyle PJ, Iglesias MA, Watson DG, Cooney GJ, Kraegen EW. Peroxisome proliferator-activated receptor (PPAR)-alpha activation lowers muscle lipids and improves insulin sensitivity in high fat-fed rats: comparison with PPAR-gamma activation. Diabetes. 2001 Feb;50(2):411-7. |
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| Cas No. | 50892-23-4 | SDF | |
| 别名 | 匹立尼酸,WY 14643,WY14643 | ||
| 化学名 | 2-[4-chloro-6-(2,3-dimethylanilino)pyrimidin-2-yl]sulfanylacetic acid | ||
| Canonical SMILES | CC1=C(C(=CC=C1)NC2=CC(=NC(=N2)SCC(=O)O)Cl)C | ||
| 分子式 | C14H14ClN3O2S | 分子量 | 323.8 |
| 溶解度 | ≥ 16.2 mg/mL in DMSO, ≥ 48.8 mg/mL in EtOH with ultrasonic | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet