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WY-14643 (Pirinixic Acid)

Catalog No.
A4305
PPARα agonist,selective and highly potent
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$77.00
In stock
50mg
$74.00
In stock
250mg
$239.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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

Laura Popescu, Oliver Rau, Jark B?ttcher, 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

Heiko Zettl, Michaela Dittrich, Ramona Steri, Ewgenij Proschak, Oliver Rau, Dieter Steinhilber, Gisbert Schneider, Michael L?mmerhofer, 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

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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt323.8
Cas No.50892-23-4
FormulaC14H14ClN3O2S
SynonymsWY 14643,WY14643
Solubilityinsoluble in H2O; ≥16.2 mg/mL in DMSO; ≥48.8 mg/mL in EtOH with ultrasonic
Chemical Name2-[4-chloro-6-(2,3-dimethylanilino)pyrimidin-2-yl]sulfanylacetic acid
SDFDownload SDF
Canonical SMILESCC1=C(C(=CC=C1)NC2=CC(=NC(=N2)SCC(=O)O)Cl)C
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

Human ECs and U937 cells

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.

Reacting condition

0, 2.5, 25 or 250 μM; 24 hrs

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]:

Animal models

High fat-fed rats

Dosage form

3 mg/kg/day; p.o.; for 2 weeks

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.

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.

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.

Biological Activity

Description WY-14643 is a highly potent agonist of PPARα with IC50 value of 10.11 μM for human PPARα.
Targets PPARα          
IC50 10.11 μM (human)          

Quality Control