L-165041
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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 402.44 |
Cas No. | 79558-09-1 |
Formula | C22H26O7 |
Synonyms | L 165041;L165041 |
Solubility | ≥40.2 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 2-[4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]phenoxy]acetic acid |
SDF | Download SDF |
Canonical SMILES | CCCC1=C(C=CC(=C1O)C(=O)C)OCCCOC2=CC=C(C=C2)OCC(=O)O |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Description | L-165041 is a potent agonist of PPARδ with Ki value of 6 nM. | |||||
Targets | PPARδ | |||||
IC50 | 6 nM (Ki) |
Quality Control & MSDS
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Chemical structure
