WY-14643 (Pirinixic Acid) (Synonyms: NSC 310038, Pirinixic Acid) |
| Katalog-Nr.GC14403 |
PPAR activator
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Überlieferungen | NSC 310038, Pirinixic Acid | ||
| Chemical Name | 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 | ||
| Formula | C14H14ClN3O2S | M.Wt | 323.8 |
| Löslichkeit | ≥ 16.2 mg/mL in DMSO, ≥ 48.8 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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