L-165041

Short Summary : PPARβ/δ agonist,cell permeable,potent and selective

Category : Metabolism|PPAR

Purity : 0.9807

CAS Number : 79558-09-1

Formula : C22H26O7

Molecular Weight : 402.44

SMILE : CCCC1=C(C=CC(=C1O)C(=O)C)OCCCOC2=CC=C(C=C2)OCC(=O)O

Solubility : >40.2mg/mL in DMSO

Storage : Store at -20°C

Description : Ki: 6 nM for PPARPeroxisome proliferator-activated receptor (PPAR) is known to be expressed ubiquitously and involved in lipid and glucose metabolism. Studies have demonstrated that PPAR is expressed in endothelial cells and plays a potential role in endothelial proliferation and survival. L-165041 is reported as a selective and potent PPAR ligand.In vitro: L-165041, which is a selective and potent PPARligand, displayed in this specified transactivation system, apart from its highly efficacious PPAR agonist activity, partial and full agonism at, respectively, PPAR2 and PPARsubtypes [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 PPAR, apolipoprotein B, IL-1, and interleukin-6. In contrast, L-165041 increased hepatic expressions of PPAR, 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.

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