product name WY-14643 (Pirinixic Acid)
Description: WY 14643 (also known as Pirinixic Acid) is a potent and selective peroxisome proliferator and activator of PPARα with EC50 of 1.5 μM. WY-14643 negatively inhibits NF-κB transcriptional activity and decreases the inflammatory response in vitro and in vivo. It is shown that aliphatic α-substitution of WY-14643 enhances both PPARα and PPARγ agonism.
References: Nature. 1990 Oct 18;347(6294):645-50; Nature. 1998 Jun 25;393(6687):790-3; FASEB J. 2002 Jul;16(9):1027-40.
323.8
Formula
C14H14ClN3O2S
CAS No.
50892-23-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 65 mg/mL (200.7 mM)
Water: <1 mg/mL
Ethanol: 65 mg/mL (200.7 mM)
Solubility (In vivo)
Synonyms
NSC 310038
other peoduct :
| In Vitro |
In vitro activity: WY 14643 (10 μM) almost completely inhibits interleukin-1-induced production of interleukin-6 and prostaglandin and expression of cyclooxygenase-2 in aortic smooth-muscle cells, through repression of NF-κB signaling. WY14643 (250 μM) reduces VCAM-1 expression levels significantly, to 52 % of TNF-α-stimulated human endothelial cells. Pretreatment of endothelial cells with WY 14643 (10 μM) before TNF-α stimulation reduces U937 cell adhesion by 50%. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | WY 14643 (1 mg/kg i.v. bolus) administration at 30 min before left anterior descending occlusion, causes significant reduction in infarct size of ∼44% in rats subjected to regional myocardial ischemia (25 min) and reperfusion (2 h). WY 14643 (3 mg/kg) lowers basal plasma levels of glucose, triglycerides (-16% vs. untreated), and leptin (-52%), and also muscle triglyceride (-34%) and total long-chain acyl-CoAs (LCACoAs) (-41%) in high fat-fed rats. WY14643 substantially reduces visceral fat weight and total liver triglyceride content without increasing body weight gain. WY14643 enhances whole body insulin sensitivity (clamp glucose infusion rate increases 35% and glucose disposals 22%, vs. untreated). WY 14643 enhances insulin-mediated muscle glucose metabolic index (Rg) in red (47%) and white (63%) muscles as well as in white adipose tissue (90%), and reduces muscle triglyceride and LCACoA accumulation. |
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| References | Nature. 1990 Oct 18;347(6294):645-50; Nature. 1998 Jun 25;393(6687):790-3; FASEB J. 2002 Jul;16(9):1027-40. |
