Name: WY-14643 (Pirinixic Acid)
Brand: Selleck Chemicals
SKU: S8029
Rating: 5 (16 reviews)

WY-14643 (Pirinixic Acid, NSC 310038) is a potent and selective PPARα activator with an EC50 of 1.5 μM.

WY-14643 (Pirinixic Acid) Chemical Structure

CAS: 50892-23-4

Selleck's WY-14643 (Pirinixic Acid) has been cited by 16 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.91%

99.91

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Signaling Pathway

PPAR Signaling Pathway

Choose Selective PPAR Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
Hep G2 cells	Function assay			Agonist activity at mouse PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay, EC50=0.04 μM	19053776
MCF7 cells	Function assay			Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 6 hrs by luciferase reporter gene assay, EC50=0.542 μM	24936232
U2OS cells	Function assay			Agonist activity at human PPARalpha in U2OS cells by transactivation assay, EC50=12 μM	18329751
HEK293 cells	Function assay			Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay, EC50=23.33 μM	23265844
COS7 cells	Function assay			Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay, IC50=36.3 μM	25037914
EAhy926 cells	Function assay	10 uM	12 h	Inhibition of tube formation in human EAhy926 cells at 10 uM pre-incubated for 12 hrs measured after 24 hrs by phase-contrast microscopy	19036594
mouse NIH3T3 cells	Function assay	0.1-10 μM		Transactivation of mouse recombinant PPARalpha expressed in mouse NIH3T3 cells at 0.1 uM to 10 uM by PPRE activation based dual luciferase reporter gene assay relative to control	19237283
HepaR cells	Function assay	25 μM	1 day	Agonist activity at PPARalpha in human HepaR cells assessed as increase in HMGCS2 gene expression at 25 uM incubated for 1 day by quantitative PCR method relative to untreated control	25497132
Click to View More Cell Line Experimental Data

Biological Activity

Description

WY-14643 (Pirinixic Acid, NSC 310038) is a potent and selective PPARα activator with an EC50 of 1.5 μM.

Targets

PPARα ^[1]

1.5 μM(EC50)

In vitro
In vitro	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. ^[2] 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%. ^[3]

In Vivo
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). ^[4] 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. ^[5]

References

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Chemical Information & Solubility

Molecular Weight	323.8	Formula	C₁₄H₁₄ClN₃O₂S
CAS No.	50892-23-4	SDF	Download WY-14643 (Pirinixic Acid) SDF
Smiles	CC1=C(C(=CC=C1)NC2=CC(=NC(=N2)SCC(=O)O)Cl)C
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 64 mg/mL ( (197.65 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 64 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5% DMSO 1 95% Corn oil	0.6mg/ml (1.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	6.25mg/ml (19.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 125 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.25mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL 65 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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