MG L-165;041 1PC x 5MG

Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target K_i: 6 nM for hPPARδ and 730 nM for hPPARγ

Primary TargetPeroxisome proliferator activator receptor δ (PPAR@delta;)

Cell permeable: yes

General description

A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor δ (PPARδ) agonist (K_i = 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.

A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor δ (PPARδ) agonist (K_i = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Rival, Y., et al. 2002. Eur. J. Pharmacol.435, 143.Castrillo, A., et al. 2001. J. Biol. Chem.276, 34082.Hansen, J.B., et al. 2001. J. Biol. Chem.276, 3175.Son, C., et al. 2001. Endocrinology142, 4189.Wilkie, N., et al. 2001. J. Neurochem.78, 1135.Leibowitz, M.D., et al. 2000. FEBS Lett.473, 333.Berger, J., et al. 1999. J. Biol. Chem.274, 6718.Lim, H., et al. 1999. Genes Dev.13, 1561.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

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

Warning

Toxicity: Irritant (B)