WY-14643

Cas：50892-23-4

Product Information：

WY-14643, also known as pirinixic acid, is a selective PPARα agonist. WY-14643 negatively inhibits NF-κB transcriptional activity and decreases the inflammatory response in vitro and in vivo.

Chemical Formula: C14H14ClN3O2S

Exact Mass: 323.04953

Molecular Weight: 323.8 

Elemental Analysis: C, 51.93; H, 4.36; Cl, 10.95; N, 12.98; O, 9.88; S, 9.90

Synonym: 

WY-14643

WY 14643

WY14643

Pirinixic Acid

Chemical Name:

[[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]-acetic acid

InChi Key:

SZRPDCCEHVWOJX-UHFFFAOYSA-N

InChi Code:   InChI=1S/C14H14ClN3O2S/c1-8-4-3-5-10(9(8)2)16-12-6-11(15)17-14(18-12)21-7-13(19)20/h3-6H,7H2,1-2H3,(H,19,20)(H,16,17,18)

Smiles Code:

O=C(O)CSC1=NC(NC2=CC=CC(C)=C2C)=CC(Cl)=N1

Technical Data：

Appearance: White to off-white crystalline powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

In Vitro：

WY-14643 is an agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.

WY-14643 (Wy-14643; 0, 10, 100 μM) enhances protein expression of PPAR-α in synovial fibroblasts.

WY-14643 (0, 10, 100 μM) shows inhibitroy effects on NO and PGE2 production in LPS-stimulated synovial fibroblasts.

WY-14643 also effectively downregulates expression of inflammatory mediators such as VCAM-1, ICAM-1, ET-1, and TF in synovial fibroblasts, blocks LPS-induced NF-kB activation, IkB phosphorylation, and NF-kB nuclear translocation in synovial fibroblasts, but Pirinixic acid shows no effects in PPAR-α silenced cells.

In Vivo：

WY-14643 (Wy-14643; 10 mg/kg, i.v.) decreases hepatic injury and lipid peroxidation (MDA) levels in obese rats. WY-14643 also causes increased SIRT1 activity in Sham and ischemia-reperfusion (IR) group, but shows no effects on SIRT3 protein expression. WY-14643 enhances NAD+, and ATP levels, and prevents endoplasmic reticulum stress (ERS) in rats.

References：

1. Merk D, Zettl M, Steinhilber D, Werz O, Schubert-Zsilavecz M. Pirinixic acids: flexible fatty acid mimetics with various biological activities. Future Med Chem. 2015 Aug;7(12):1597-616. doi: 10.4155/fmc.15.87. Epub 2015 Aug 27. PubMed PMID: 26313377.

2. Hecker M, Behnk A, Morty RE, Sommer N, Vadasz I, Herold S, Seeger W, Mayer K. PPAR-α activation reduced LPS-induced inflammation in alveolar epithelial cells. Exp Lung Res. 2015 Sep;41(7):393-403. doi: 10.3109/01902148.2015.1046200. PubMed PMID: 26151160.

3. Revuelta-Lopez E, Cal R, Julve J, Rull A, Martínez-Bujidos M, Perez-Cuellar M, Ordonez-Llanos J, Badimon L, Sanchez-Quesada JL, Llorente-Cortes V. Hypoxia worsens the impact of intracellular triglyceride accumulation promoted by electronegative low-density lipoprotein in cardiomyocytes by impairing perilipin 5 upregulation. Int J Biochem Cell Biol. 2015 Aug;65:257-67. doi: 10.1016/j.biocel.2015.06.014. Epub 2015 Jun 19. PubMed PMID: 26096040.

4. Fiamoncini J, Lima TM, Hirabara SM, Ecker J, Gorjao R, Romanatto T, ELolimy A, Worsch S, Laumen H, Bader B, Daniel H, Curi R. Medium-chain dicarboxylic acylcarnitines as markers of n-3 PUFA-induced peroxisomal oxidation of fatty acids. Mol Nutr Food Res. 2015 Aug;59(8):1573-83. doi: 10.1002/mnfr.201400743. Epub 2015 May 26. PubMed PMID: 25913736.

5. Du WW, Liu F, Shan SW, Ma XC, Gupta S, Jin T, Spaner D, Krylov SN, Zhang Y, Ling W, Yang BB. Inhibition of Dexamethasone-induced Fatty Liver Development by Reducing miR-17-5p Levels. Mol Ther. 2015 Jul;23(7):1222-33. doi: 10.1038/mt.2015.64. Epub 2015 Apr 21. PubMed PMID: 25896250.

Products are for research use only. Not for human use.