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L-165041

In stock
Catalog No.
A3536
PPARβ/δ agonist,cell permeable,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$72.00
In stock
5mg
$65.00
In stock
10mg
$95.00
In stock
25mg
$199.00
In stock
100mg
$632.00
In stock

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Ki: 6 nM for PPARγ

Peroxisome proliferator-activated receptor (PPARγ) is known to be expressed ubiquitously and involved in lipid and glucose metabolism. Studies have demonstrated that PPARγ is expressed in endothelial cells and plays a potential role in endothelial proliferation and survival. L-165041 is reported as a selective and potent PPARγ ligand.

In vitro: L-165041, which is a selective and potent PPARδligand, displayed in this specified transactivation system, apart from its highly efficacious PPARδ agonist activity, partial and full agonism at, respectively, PPARγ2 and PPARαsubtypes [1].

In vivo: L-165041 could drastically reduce lipid accumulation in the mouse liver, decreasing total hepatic triglyceride and cholesterol content compared to the vehicle group. Gene analysis demonstrated that L-165041 lowered hepatic expression of PPARγ, apolipoprotein B, IL-1β, and interleukin-6. In contrast, L-165041 increased hepatic expressions of PPARδ, lipoprotein lipase, and ATP-binding cassette transporter G1 (ABCG1) [2].

Clinical trial: Up to now, L-165041 is still in the preclinical development stage.

Reference:
[1] Wurch T, Junquero D, Delhon A, Pauwels J.  Pharmacological analysis of wild-type alpha, gamma and delta subtypes of the human peroxisome proliferator-activated receptor. Naunyn Schmiedebergs Arch Pharmacol. 2002 Feb;365(2):133-40.
[2] Lim HJ, Park JH, Lee S, Choi HE, Lee KS, Park HY.  PPARdelta ligand L-165041 ameliorates Western diet-induced hepatic lipid accumulation and inflammation in LDLR-/- mice. Eur J Pharmacol. 2009 Nov 10;622(1-3):45-51.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt402.44
Cas No.79558-09-1
FormulaC22H26O7
SynonymsL 165041;L165041
Solubility≥40.2 mg/mL in DMSO, <2.71 mg/mL in EtOH, <2.07 mg/mL in H2O
Chemical Name2-[4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]phenoxy]acetic acid
SDFDownload SDF
Canonical SMILESCCCC1=C(C=CC(=C1O)C(=O)C)OCCCOC2=CC=C(C=C2)OCC(=O)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description L-165041 is a potent agonist of PPARδ with Ki value of 6 nM.
Targets PPARδ          
IC50 6 nM (Ki)          

Quality Control

Chemical structure

L-165041