L-165,041

别名

L-165,041 - CAS 79558-09-1 - Calbiochem,Compound P, L165041, 4-[3-(2-Propyl-3-hydroxy-4-acetyl)phenoxy]propyloxyphenoxy-acetic acid, PPAR Agonist VIII, PPARα Agonist III, PPARγ Agonist VII

一般描述

A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor δ (PPARδ) agonist (Ki = 6 nM for hPPAR δ and 730 nM for hPPARγ). Induces adipocyte differentiation in NIH-PPARδ cells at 500 nM. Also reported to raise total cholesterol in insulin-resistant db/db mice without altering glucose or triglyceride levels. Shown to increase uncoupling protein 3 (UCP3) gene expression in L6 myotubes. Also shown to inhibit cytokine-induced expression of vascular cell adhesion molecule-1 (VCAM-1) and the secretion of monocyte chemotactic protein-1 (MCP-1) in Eahy926 cells. A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor δ (PPARδ) agonist (Ki = 6 nM for hPPARδ and 730 nM for hPPARγ). Potently induces adipocyte differentiation in NIH-PPARδ cells at 500 nM and raises total cholesterol in insulin resistant db/db mice without altering glucose or triglycerides levels. Increases UCP3 (uncoupling protein 3) gene expression in L6 myotubes. Inhibits cytokine-induced expression of VCAM-1 (vascular cell adhesion molecule-1) and the secretion of MCP-1 (monocyte chemotactic protein-1) in EAhy926 cells.

生化/生理作用

Cell permeable: yes Primary Target
Peroxisome proliferator activator receptor δ (PPAR@delta;) Product does not compete with ATP. Reversible: no Target Ki: 6 nM for hPPARδ and 730 nM for hPPARγ

重悬

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

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Leibowitz, M.D., et al. 2000. FEBS Lett.473, 333.
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Lim, H., et al. 1999. Genes Dev.13, 1561.